Vevorisertib trihydrochloride(Synonyms: ARQ 751 trihydrochloride)

发表于2025年4月24日由上海金畔生物科技有限公司

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Vevorisertib trihydrochloride (Synonyms: ARQ 751 trihydrochloride) 纯度: 99.13%

Vevorisertib (ARQ 751) trihydrochloride 是选择性、变构、pan-AKT 和 AKT1-E17K 突变抑制剂，可有效抑制 AKT 的磷酸化。Vevorisertib trihydrochloride 对 AKT1 和 AKT1-E17K 的 Kd 值分别为 1.2 nM 和 8.6 nM。Vevorisertib trihydrochloride 对 AKT1、AKT2 和 AKT3 的 IC₅₀ 值分别为 0.55、0.81 和 1.3 nM。 Vevorisertib trihydrochloride 可用于癌症的研究。

Vevorisertib trihydrochloride Chemical Structure

CAS No. : 1416775-08-0

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10 mg	￥9000	In-stock
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Vevorisertib trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton Compound Library
Orally Active Compound Library
Glutamine Metabolism Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Anti-Cancer Metabolism Compound Library
Anti-Obesity Compound Library
Angiogenesis Related Compound Library
Glucose Metabolism Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC₅₀ values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer^[1].

IC₅₀ & Target^[1]

Akt1

0.55 nM (IC₅₀)

Akt2

0.81 nM (IC₅₀)

Akt3

1.31 nM (IC₅₀)

Akt1

1.2 nM (Kd)

Akt1^E17K

8.6 nM (Kd)

体外研究
(In Vitro)

Vevorisertib trihydrochloride (0, 12, 33, 111, 333, 1000 nM, 2 hours) inhibits phosphorylation of AKT1-E17K^[1].
Vevorisertib trihydrochloride (1 μM for 2 hours; NIH 3T3 cells are transfected with either pcDNAAKT-WT-GFP or pcDNA-E17K-GFP) inhibits plasma membrane translocation of AKT-WT and AKT1-E17K irrespective of the presence of growth factors^[1].
Vevorisertib trihydrochloride (5 μM) exhibites 57% inhibition of full-length AKT1^[1].
Vevorisertib trihydrochloride (0, 0.012, 0.037, 0.11, 0.33, 1 μM; 2 hours) shows a dose-dependent effect on mTORC1 and AKT direct substrates including PRAS40, GSK3β, FOXO, BAD, and AS160 in cancer cell lines^[1].
Vevorisertib trihydrochloride has anti-proliferative effect on esophageal, breast, and head and neck cancer cells (GI₅₀ < 1 μM)^[1].
Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines^[1].
Vevorisertib trihydrochloride (MK-4440)/imatinib mesylate (IM) combination shows cell cycle arrest, and increases cell death of gastrointestinal stromal tumor (GIST) cells^[2].
Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines^[1]:

Breast Cancer Cell Lines	GI₅₀ (nM)	PIK3CA	ER	PR	HER2
T47D	1.05	H1047R	+	+	–
EFM-19	1.54	H1047R	+	+	–
MCF-7	2.20	E545K	+	+	–
BT474	3.25	K111N	+	+	+
MDA-MB-453	6.05	H1047R	–	–	+

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	293T cells (transiently transfected with pcDNA-E17K-GFP)
Concentration:	0, 12, 33, 111, 333, 1000 nM
Incubation Time:	2 hours
Result:	Inhibited phosphorylation of AKT1-E17K.

Western Blot Analysis^[1]

Cell Line:	Cancer cell lines: MDA-MB 453 (PIK3CAH1047R; Her2 amp), NCI-H1650 (PTEN null), KU-19-19 (AKT1-E17K&E49K; NRas Q61R)
Concentration:	0, 0.012, 0.037, 0.11, 0.33, 1 μM
Incubation Time:	2 hours
Result:	Showed a dose-dependent effect on mTORC1 and AKT direct substrates including PRAS40, GSK3β, FOXO, BAD, and AS160.

体内研究
(In Vivo)

Vevorisertib trihydrochloride (25, 50 and 75 mg/kg; p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days) shows potent tumor growth inhibition of 68, 78 and 98%, respectively^[1].
Vevorisertib trihydrochloride (5, 10, 20, 40, 80, and 120 mg/kg; p.o. daily for ten days) shows tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively^[1].
Vevorisertib trihydrochloride reachs C_max plasma concentrations of ≥2 μM^[1].
Vevorisertib trihydrochloride is generally well-tolerated at dose levels up to 120 mg/kg^[1].
Vevorisertib trihydrochloride (MK-4440)/IM combination shows superior efficacy in an IM-sensitive preclinical model of GIST compared with either single agent^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Endometrial PDX mouse xenograft models (AKT1-E17K mutation tumor fragments subcutaneously implanted in athymic nude mice; tumor volume of approximately 200 mm³)^[1]
Dosage:	25, 50 and 75 mg/kg
Administration:	p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days
Result:	Showed potent tumor growth inhibition of 68, 78 and 98%, respectively.

Animal Model:	AN3CA mouse xenograft models (female NCr nu/nu mice with 250 mm³ tumors size)^[1]
Dosage:	5, 10, 20, 40, 80, and 120 mg/kg
Administration:	p.o.; daily for ten days
Result:	Showed tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively.

分子量

696.11

Formula

C₃₅H₄₁Cl₃N₈O

CAS 号

1416775-08-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 150 mg/mL (215.48 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4366 mL	7.1828 mL	14.3655 mL
5 mM	0.2873 mL	1.4366 mL	2.8731 mL
10 mM	0.1437 mL	0.7183 mL	1.4366 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 5.25 mg/mL (7.54 mM); Clear solution

此方案可获得 ≥ 5.25 mg/mL (7.54 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 5.25 mg/mL (7.54 mM); Clear solution

此方案可获得 ≥ 5.25 mg/mL (7.54 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 52.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Yu Y, et al. Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092. PLoS One. 2015 Oct 15;10(10):e0140479.

[2]. Kozinova M, et al. Combined Inhibition of AKT and KIT Restores Expression of Programmed Cell Death 4 (PDCD4) in Gastrointestinal Stromal Tumor. Cancers (Basel). 2021 Jul 23;13(15):3699.

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CBB1007 trihydrochloride

发表于2025年3月28日由上海金畔生物科技有限公司

CBB1007 trihydrochloride 纯度: 96.58%

CBB1007三盐酸盐是LSD1选择性抑制剂，IC50值为5.27uM。

CBB1007 trihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3294	In-stock
2 mg	￥1550	In-stock
5 mg	￥2325	In-stock
10 mg	￥3534	In-stock
50 mg	￥8370	In-stock
100 mg	￥13020	In-stock
200 mg		询价
500 mg		询价

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CBB1007 trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library

生物活性

CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1). IC50 Value: 5.27 uM Target: hLSD1 CBB1007 efficiently can block LSD1-mediated demethylation of H3K4Me2 and H3K4Me (IC50 ≤ 5 μM) with no effect on H3K4Me3 and H3K9Me2, and LSD2 and JARID1A activities. Increases H3K4Me2 and H3K4Me contents (IC50 ≤ 5 μM), and causes activation of epigenetically suppressed CHRM4/M4-ArchR and SCN3A genes in F9 cells (IC50 ≤ 3.74 μM). CBB1007 was Shown to preferentially arrest the growth of pluripotent tumors with minimal effect on non-pluripotent cancer or normal somatic cells (IC50 ≥ 100 μM).

分子量

643.99

Formula

C₂₇H₃₇Cl₃N₈O₄

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 54 mg/mL (83.85 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5528 mL	7.7641 mL	15.5282 mL
5 mM	0.3106 mL	1.5528 mL	3.1056 mL
10 mM	0.1553 mL	0.7764 mL	1.5528 mL

参考文献

[1]. Wang J, et al. Novel histone demethylase LSD1 inhibitors selectively target cancer cells with pluripotent stem cell properties. Cancer Res. 2011 Dec 1;71(23):7238-49.

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HM03 trihydrochloride

发表于2025年2月16日由上海金畔生物科技有限公司

HM03 trihydrochloride

HM03 trihydrochloride是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip，Grp78) 抑制剂，具有抗肿瘤活性。

HM03 trihydrochloride Chemical Structure

CAS No. : 1082532-95-3

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HM03 trihydrochloride 的其他形式现货产品:

HM03

生物活性	HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity^[1].
体外研究 (In Vitro)	HM03 trihydrochloride (0.1-50 μM; 72 hours) exhibits over 50% inhibition at 25 µM concentration in HCT116 cells^[1]. HM03 trihydrochloride forms more binding interactions with HSPA5 and HSPA9 than with the other HSP70 proteins^[1]. HM03 trihydrochloride exhibits promising inhibition activities from cancer cell viability and tumor inhibition assays^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	572.35
Formula	C₂₆H₃₀Cl₄N₄O₂
CAS 号	1082532-95-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Huang M, et al. Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors. Bioorg Med Chem Lett. 2013;23(10):3044-3050.

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HM03 trihydrochloride

发表于2025年2月16日由上海金畔生物科技有限公司

HM03 trihydrochloride

HM03 trihydrochloride是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip，Grp78) 抑制剂，具有抗肿瘤活性。

HM03 trihydrochloride Chemical Structure

CAS No. : 1082532-95-3

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

HM03 trihydrochloride 的其他形式现货产品:

HM03

生物活性	HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity^[1].
体外研究 (In Vitro)	HM03 trihydrochloride (0.1-50 μM; 72 hours) exhibits over 50% inhibition at 25 µM concentration in HCT116 cells^[1]. HM03 trihydrochloride forms more binding interactions with HSPA5 and HSPA9 than with the other HSP70 proteins^[1]. HM03 trihydrochloride exhibits promising inhibition activities from cancer cell viability and tumor inhibition assays^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	572.35
Formula	C₂₆H₃₀Cl₄N₄O₂
CAS 号	1082532-95-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Huang M, et al. Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors. Bioorg Med Chem Lett. 2013;23(10):3044-3050.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

HM03 trihydrochloride

发表于2025年2月16日由上海金畔生物科技有限公司

HM03 trihydrochloride

HM03 trihydrochloride是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip，Grp78) 抑制剂，具有抗肿瘤活性。

HM03 trihydrochloride Chemical Structure

CAS No. : 1082532-95-3

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

HM03 trihydrochloride 的其他形式现货产品:

HM03

生物活性	HM03 trihydrochloride is a potent and selective HSPA5 (Heat shock 70kDa protein 5, also known as Bip, Grp78) inhibitor. HM03 trihydrochloride has anticancer activity^[1].
体外研究 (In Vitro)	HM03 trihydrochloride (0.1-50 μM; 72 hours) exhibits over 50% inhibition at 25 µM concentration in HCT116 cells^[1]. HM03 trihydrochloride forms more binding interactions with HSPA5 and HSPA9 than with the other HSP70 proteins^[1]. HM03 trihydrochloride exhibits promising inhibition activities from cancer cell viability and tumor inhibition assays^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	572.35
Formula	C₂₆H₃₀Cl₄N₄O₂
CAS 号	1082532-95-3
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Huang M, et al. Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors. Bioorg Med Chem Lett. 2013;23(10):3044-3050.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

ARN5187 trihydrochloride

发表于2024年11月30日由上海金畔生物科技有限公司

ARN5187 trihydrochloride

ARN5187 trihydrochloride 是一种亲溶酶体 REV-ERBβ 配体，抑制 REV-ERB 介导的转录调控和细胞自噬。ARN5187 trihydrochloride 显示出溶酶体效力和细胞毒性。ARN5187 trihydrochloride 诱导细胞凋亡 (apoptosis)。

ARN5187 trihydrochloride Chemical Structure

CAS No. : 1700693-96-4

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生物活性

ARN5187 trihydrochloride is a lysosomotropic REV-ERBβ ligand with a dual inhibitory activity toward REV-ERB-mediated transcriptional regulation and autophagy. ARN5187 trihydrochloride shows lysosomotropic potency and cytotoxicity. ARN5187 trihydrochloride induces apoptosis^[1]^[2].

IC₅₀ & Target

REV-ERBβ^[1]

体外研究
(In Vitro)

ARN5187 trihydrochloride (compound 1) (0-100 µM; 48 h) shows cytotoxicity with EC₅₀ of 23.5 µM in BT-474 cells and IC₅₀ of 30.14 µM, >100 µM for BT-474 and HMEC cells, respectively^[1]^[2].
ARN5187 trihydrochloride (0-100 µM) activates the RevRE reporter in a concentration-dependent manner in HEK-293 cells^[1].
ARN5187 trihydrochloride (25, 50 µM) is a lysosomotropic-independent REV-ERB antagonistic activity^[1].
ARN5187 trihydrochloride (50 µM; 24 h) shows autophagy inhibition^[1].
ARN5187 trihydrochloride (50 µM; 2, 8, 24 h) effects autophagy formation and maturation^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:	BT-474 cells
Concentration:	0-100 µM
Incubation Time:	48 h
Result:	Showed cytotoxicity with EC₅₀ of 23.5 µM.

Western Blot Analysis^[1]

Cell Line:	BT-474 cells
Concentration:	50 µM
Incubation Time:	24 h
Result:	Significantly increased the expression of α-LC3-II, α-p62, α-Cleaved PARP.

RT-PCR^[1]

Cell Line:	BT-474 cells
Concentration:	25, 50 µM
Incubation Time:
Result:	Significantly enhanced the expression of BMAL1, PER1 and PEPCK in a dose-dependent manner.

分子量

506.91

Formula

C₂₄H₃₅Cl₃FN₃O

CAS 号

1700693-96-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. De Mei C, et al. Dual inhibition of REV-ERBβ and autophagy as a novel pharmacological approach to induce cytotoxicity in cancer cells. Oncogene. 2015 May 14;34(20):2597-608.

[2]. Torrente E, et al. Synthesis and in Vitro Anticancer Activity of the First Class of Dual Inhibitors of REV-ERBβ and Autophagy. J Med Chem. 2015 Aug 13;58(15):5900-15.

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Tazemetostat trihydrochloride(Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

发表于2024年10月30日由上海金畔生物科技有限公司

Tazemetostat trihydrochloride (Synonyms: EPZ-6438 trihydrochloride; E-7438 trihydrochloride)

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat trihydrochloride 抑制含有 PRC2 复合体的野生型 EZH2 的活性， K_i 值为 2.5 nM。Tazemetostat trihydrochloride 抑制 EZH2，在肽测定和核小体测定中 IC₅₀ 分别为 11 和 16 nM。Tazemetostat trihydrochloride 抑制大鼠 EZH2，IC₅₀ 为 4 nM。Tazemetostat trihydrochloride 还抑制 EZH1，IC₅₀ 为 392 nM。

Tazemetostat trihydrochloride Chemical Structure

CAS No. : 1403255-00-4

规格		是否有货
100 mg		询价
250 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Tazemetostat trihydrochloride 的其他形式现货产品:

Tazemetostat Tazemetostat hydrobromide

生物活性

Tazemetostat trihydrochloride (EPZ-6438 trihydrochloride) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat trihydrochloride inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i of 2.5 nM. Tazemetostat trihydrochloride inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat trihydrochloride inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC₅₀ of 392 nM^[1].

IC₅₀ & Target^[1]

EZH2 WT

2.5 nM (Ki)

EZH2

11 nM (IC₅₀, in peptide assay)

EZH2

16 nM (IC₅₀, in nucleosome assay)

Rat EZH2

4 nM (IC₅₀)

EZH1

392 nM (IC₅₀)

体外研究
(In Vitro)

Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC₅₀s of 0.49 nM-7.6 μM^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
Concentration:	0.49 nM-7.6 μM
Incubation Time:	11 days
Result:	Inhibited DOHH-2 cell (EZH2 wild-type; IC₅₀=1.7 μM), Farage cell (EZH2 wild-type; IC₅₀=99 nM), OCI-LY19 cell (EZH2 wild-type; IC₅₀=6.2 μM), Toledo cell (EZH2 wild-type; IC₅₀=7.6 μM), KARPAS-422 (EZH2 Y646N; IC₅₀=1.8 nM), Pfeiffer (EZH2 A682G; IC₅₀=0.49 nM), RL cell line (EZH2 Y646N; IC₅₀=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC₅₀=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC₅₀=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC₅₀=8.6 nM) proliferation.

体内研究
(In Vivo)

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice bearing s.c. G401 xenografts^[1]
Dosage:	125 mg/kg, 250 mg/kg, 500 mg/kg
Administration:	Oral; twice daily; 28 days
Result:	Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.

Clinical Trial

分子量

682.12

Formula

C₃₄H₄₇Cl₃N₄O₄

CAS 号

1403255-00-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Knutson SK, et al. Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferaseEZH2. Proc Natl Acad Sci U S A. 2013 May 7;110(19):7922-7.

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DMA trihydrochloride

发表于2024年10月24日由上海金畔生物科技有限公司

DMA trihydrochloride 纯度: 98.01%

DMA trihydrochloride 是一种荧光化合物 (λ_ex=340 nm, λ_em=478 nm)。

DMA trihydrochloride Chemical Structure

CAS No. : 2095832-33-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in Water	￥763	In-stock
5 mg	￥600	In-stock
10 mg	￥900	In-stock
25 mg	￥2000	In-stock
50 mg	￥3600	In-stock
100 mg	￥6600	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

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Bioactive Compound Library Plus
Anti-Cancer Compound Library

生物活性

DMA trihydrochloride is a fluorescent compound (λ_ex=340 nm, λ_em=478 nm).

IC₅₀ & Target

IC50: 3.4 μM (HeLa cell), 5.3 μM (MCF7 cell)^[1]

体外研究
(In Vitro)

The newly synthesized bisbenzimidazole derivatives DMA (6c) is evaluated for their cytotoxicity against human tumor cell lines, which are cervix carcinoma cell line (HeLa), breast carcinoma cell line (MCF7) and brain glioma cell line (U87) in comparison to Hoechst. In case of MCF7, the IC₅₀ is observed at 5.3 μM for DMA. The IC₅₀ determined in the case of HeLa is 3.4 μM for DMA^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

577.93

Formula

C₂₇H₃₁Cl₃N₆O₂

CAS 号

2095832-33-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

H₂O : 15.9 mg/mL (27.51 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7303 mL	8.6516 mL	17.3031 mL
5 mM	0.3461 mL	1.7303 mL	3.4606 mL
10 mM	0.1730 mL	0.8652 mL	1.7303 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

参考文献

[1]. Singh M, et al. Synthesis and biological activity of novel inhibitors of topoisomerase I: 2-aryl-substituted 2-bis-1H-benzimidazoles. Eur J Med Chem. 2011 Feb;46(2):659-69.

Cell Assay	Various human tumor cells (U87, HeLa and MCF7) are maintained as monolayer at 37°C in 5% CO₂ using DMEM medium. Approximately 3000-8000 cells/well are seeded in 96-well plates containing 200 μL of medium and incubated for 24 h. The culture medium is replaced by fresh medium containing 1, 10, 50, 100 μM of DMA (6c) and incubated for 24, 48 and 72 h. The cell viability is determined by the MTT assay. The light absorbance is measured using a microplate reader^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Singh M, et al. Synthesis and biological activity of novel inhibitors of topoisomerase I: 2-aryl-substituted 2-bis-1H-benzimidazoles. Eur J Med Chem. 2011 Feb;46(2):659-69.

Cell Assay

Various human tumor cells (U87, HeLa and MCF7) are maintained as monolayer at 37°C in 5% CO₂ using DMEM medium. Approximately 3000-8000 cells/well are seeded in 96-well plates containing 200 μL of medium and incubated for 24 h. The culture medium is replaced by fresh medium containing 1, 10, 50, 100 μM of DMA (6c) and incubated for 24, 48 and 72 h. The cell viability is determined by the MTT assay. The light absorbance is measured using a microplate reader^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Singh M, et al. Synthesis and biological activity of novel inhibitors of topoisomerase I: 2-aryl-substituted 2-bis-1H-benzimidazoles. Eur J Med Chem. 2011 Feb;46(2):659-69.

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BI-9321 trihydrochloride

发表于2024年10月23日由上海金畔生物科技有限公司

BI-9321 trihydrochloride 纯度: 98.89%

BI-9321 trihydrochloride 是一种有效的，选择性的，具有细胞活性的 NSD3-PWWP1 拮抗剂，K_d 值为 166 nM。BI-9321 对 NSD2-PWWP1 和 NSD3-PWWP2 无效。BI-9321 trihydrochloride 在 U2OS 细胞中特异性破坏 NSD3-PWWP1 与组蛋白相互作用，IC₅₀ 为 1.2 μM。

BI-9321 trihydrochloride Chemical Structure

CAS No. : 2387510-87-2

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1430	In-stock
5 mg	￥1300	In-stock
10 mg	￥2300	In-stock
25 mg	￥4500	In-stock
50 mg	￥7600	In-stock
100 mg	￥12000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

BI-9321 trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Anti-Blood Cancer Compound Library
Targeted Diversity Library

生物活性

BI-9321 trihydrochloride is a potent, selective and cellular active nuclear receptor-binding SET domain 3 (NSD3)-PWWP1 domain antagonist with a K_d value of 166 nM. BI-9321 trihydrochloride is inactive against NSD2-PWWP1 and NSD3-PWWP2. BI-9321 trihydrochloride specifically disrupts histone interactions of the NSD3-PWWP1 domain with an IC₅₀ of 1.2 μM in U2OS cells^[1].

IC₅₀ & Target

Kd: 166 nM (NSD3-PWWP1)^[1]

体外研究
(In Vitro)

BI-9321 trihydrochloride is targeting the methyl-lysine binding site of the PWWP1 domain with sub-micromolar in vitro activity and cellular target engagement at 1 µM. As a single agent, BI-9321 trihydrochloride downregulates Myc messenger RNA expression and reduces proliferation in MOLM-13 cells^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

469.81

Formula

C₂₂H₂₄Cl₃FN₄

CAS 号

2387510-87-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (532.13 mM; Need ultrasonic)

H₂O : 25 mg/mL (53.21 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1285 mL	10.6426 mL	21.2852 mL
5 mM	0.4257 mL	2.1285 mL	4.2570 mL
10 mM	0.2129 mL	1.0643 mL	2.1285 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 25 mg/mL (53.21 mM); Clear solution

此方案可获得 ≥ 25 mg/mL (53.21 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 250.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Böttcher J, et al. Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3. Nat Chem Biol. 2019 Aug;15(8):822-829.

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NSC 23766 trihydrochloride

发表于2024年10月16日由上海金畔生物科技有限公司

NSC 23766 trihydrochloride 纯度: 99.66%

NSC 23766 trihydrochloride 是 Rac1 激活的抑制剂。

NSC 23766 trihydrochloride Chemical Structure

CAS No. : 1177865-17-6

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥584	In-stock
5 mg	￥500	In-stock
10 mg	￥880	In-stock
50 mg	￥3760	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

NSC 23766 trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
GPCR/G Protein Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Diabetes Related Compound Library
Ferroptosis Compound Library
Glutamine Metabolism Compound Library
Anti-Pancreatic Cancer Compound Library
Anti-Blood Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

NSC 23766 trihydrochloride is an inhibitor of Rac1 activation.

体外研究
(In Vitro)

NSC 23766 (100 μM) treatment effectively inhibits polar body emission in a dose-dependent manner. NSC 23766 (200 μM) increases the percentage of morphologically abnormal spindles of oocytes. In NSC 23766-treated oocytes, the p-MAPK protein expression is significantly decreased^[2]. NSC23766 (50 μM) plus 100 ng/mL Jagged1, GDF9 and BMP15, reduces the number of germLine cell cysts and increases the number of primordial follicles^[3]. NSC23766 significantly inhibits GTP-Rac1 activity and phosphorylation of Rac1-PAK, ERKs and p38 MAPK in the spinal dorsal horn neurons^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NSC23766 (2.5 mg/kg/day, i.p.) significantly attenuates the onset of spontaneous diabetes in NOD mice, without significant effects on the growth (body weights) of the mice. NSC23766 significantly increases the expression of Rac1 and CHOP, a marker for ER-stress, in islets from NOD mice^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

530.96

Formula

C₂₄H₃₈Cl₃N₇

CAS 号

1177865-17-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 33.33 mg/mL (62.77 mM; Need ultrasonic)

H₂O : ≥ 32 mg/mL (60.27 mM)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8834 mL	9.4169 mL	18.8338 mL
5 mM	0.3767 mL	1.8834 mL	3.7668 mL
10 mM	0.1883 mL	0.9417 mL	1.8834 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： PBS

Solubility: 110 mg/mL (207.17 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.71 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.71 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Veluthakal R, et al. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7.

[2]. Song SJ, et al. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415

[3]. Zhao L, et al. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972

[4]. Wang Y, et al. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50

Kinase Assay ^[4]	Briefly, fresh spinal cord tissue of the lumbar enlargement is homogenised in the presence of protease and phosphatase inhibitors and lysed with buffer. After being centrifuged at 12,000× g for 5 min at 4°C, the supernatants are collected and incubated with PAK-PBD beads at 4°C on a rotator for 1 h and then the beads are pelleted through centrifugation at 5000× g for 3 min at 4°C. The resulting pellet is resuspended in LaemmLi buffer and boiled for 2 min. The bead samples are subjected to Western blot analysis. Total Rac1 in each sample is also determined by Western blot analysis. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Balb/c control and NOD mice are at 7 weeks of age and are divided into four groups (n=8/group). At 8 weeks of age two groups of experimental animals (Balb/c and NOD) receive NSC23766 (2.5 mg/kg/day, i.p./daily) and other two groups, which serve as control Balb/c and NOD mice and receive equal volume of saline. The body weights and blood glucose are monitored every week for 34 weeks. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Veluthakal R, et al. NSC23766, a Known Inhibitor of Tiam1-Rac1 Signaling Module, Prevents the Onset of Type 1 Diabetes in the NOD Mouse Model. Cell Physiol Biochem. 2016;39(2):760-7. [2]. Song SJ, et al. Inhibition of Rac1 GTPase activity affects porcine oocyte maturation and early embryo development. Sci Rep. 2016 Oct 3;6:34415 [3]. Zhao L, et al. Rac1 modulates the formation of primordial follicles by facilitating STAT3-directed Jagged1, GDF9 and BMP15 transcription in mice. Sci Rep. 2016 Apr 6;6:23972 [4]. Wang Y, et al. Involvement of Rac1 signalling pathway in the development and maintenance of acute inflammatory pain induced by bee venom injection. Br J Pharmacol. 2016 Mar;173(5):937-50

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CM-579 trihydrochloride

发表于2024年9月27日由上海金畔生物科技有限公司

CM-579 trihydrochloride 纯度: 98.02%

CM-579 trihydrochloride 是首创的、可逆的，G9a 和DNA 甲基转移酶 (DNMT) 的双抑制剂，其IC₅₀ 值分别为 16 nM 和32 nM。在多种癌细胞中发挥有效活性作用。

CM-579 trihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3311	In-stock
5 mg	￥2500	In-stock
10 mg	￥3900	In-stock
50 mg	￥11000	In-stock
100 mg	￥15000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

CM-579 trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC₅₀ values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells^[1].

IC₅₀ & Target

DNA Methyltransferase

32 nM (IC₅₀)

DNMT1

1.5 nM (Kd)

DNMT3A

92 nM (IC₅₀)

DNMT3B

1000 nM (IC₅₀)

G9a

16 nM (IC₅₀)

体外研究
(In Vitro)

The K_d of CM-579 for DNMT1 is 1.5 nM, CM-579 also inhibits DNMT3A and DNMT3B, with IC₅₀s of 92 nM and 1000 nM, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

602.04

Formula

C₂₉H₄₃Cl₃N₄O₃

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据

In Vitro:

H₂O : 37.5 mg/mL (62.29 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (55.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6610 mL	8.3051 mL	16.6102 mL
5 mM	0.3322 mL	1.6610 mL	3.3220 mL
10 mM	0.1661 mL	0.8305 mL	1.6610 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.15 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. San José-Enériz E, et al. Discovery of first-in-class reversible dual small molecule inhibitors against G9a and DNMTs in hematological malignancies. Nat Commun. 2017 May 26;8:15424.

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Laduviglusib trihydrochloride(Synonyms: CHIR-99021 trihydrochloride; CT99021 trihydrochloride)

发表于2024年9月11日由上海金畔生物科技有限公司

Laduviglusib trihydrochloride (Synonyms: CHIR-99021 trihydrochloride; CT99021 trihydrochloride) 纯度: 98.68%

Laduviglusib (CHIR-99021) trihydrochloride 是一种有效的选择性 GSK-3α/β 抑制剂，IC₅₀ 为 10 nM 和 6.7 nM。CHIR-99021 trihydrochloride 对 GSK-3 的选择性比 CDC2，ERK2 和其他蛋白激酶高 500 倍以上。Laduviglusib trihydrochloride 还是一种有效的 Wnt/β-catenin 信号通路激活剂。Laduviglusib trihydrochloride 可增强小鼠和人类胚胎干细胞的自我更新。Laduviglusib trihydrochloride 能诱导细胞自噬 (autophagy)。

Laduviglusib trihydrochloride Chemical Structure

CAS No. : 1782235-14-6

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10 mM * 1 mL in DMSO	￥1214	In-stock
2 mg	￥650	In-stock
5 mg	￥960	In-stock
10 mg	￥1560	In-stock
50 mg	￥5880	In-stock
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生物活性

Laduviglusib (CHIR-99021) trihydrochloride is a potent and selective GSK-3α/β inhibitor with IC₅₀s of 10 nM and 6.7 nM. Laduviglusib trihydrochloride shows >500-fold selectivity for GSK-3 over CDC2, ERK2 and other protein kinases. Laduviglusib trihydrochloride is also a potent Wnt/β-catenin signaling pathway activator. Laduviglusib trihydrochloride enhances mouse and human embryonic stem cells self-renewal. Laduviglusib trihydrochloride induces autophagy^[1]^[2]^[3].

IC₅₀ & Target^[1]

GSK-3β

6.7 nM (IC₅₀)

GSK-3α

10 nM (IC₅₀)

cdc2

8800 nM (IC₅₀)

体外研究
(In Vitro)

Laduviglusib trihydrochloride inhibits human GSK-3β with K_i values of 9.8 nM^[1]. Laduviglusib trihydrochloride is a small organic molecule that inhibits GSK3α and GSK3β by competing for their ATP-binding sites.In vitro kinase assays reveal that Laduviglusib trihydrochloride specifically inhibits GSK3β (IC₅₀=~5 nM) and GSK3α (IC₅₀=~10 nM), with little effect on other kinases^[4]. In the presence of Laduviglusib trihydrochloride the viability of the ES-D3 cells is reduced by 24.7% at 2.5 μM, 56.3% at 5 μM, 61.9% at 7.5 μM and 69.2% at 10 μM Laduviglusib trihydrochloride with an IC₅₀ of 4.9 μM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In ZDF rats, a single oral dose of Laduviglusib (16 mg/kg or 48 mg/kg) trihydrochloride rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration^[1]. Laduviglusib (2 mg/kg) trihydrochloride given once, 4 h before irradiation, significantly improves survival after 14.5 Gy abdominal irradiation (ABI). Laduviglusib trihydrochloride treatment significantly blocks crypt apoptosis and accumulation of p-H2AX⁺ cells, and improves crypt regeneration and villus height. Laduviglusib trihydrochloride treatment increases Lgr5⁺ cell survival by blocking apoptosis, and effectively prevents the reduction of Olfm4, Lgr5 and CD44 as early as 4 h^[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

574.72

Formula

C₂₂H₂₁Cl₅N₈

CAS 号

1782235-14-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : ≥ 32 mg/mL (55.68 mM)

H₂O : 19 mg/mL (33.06 mM; Need ultrasonic and warming)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7400 mL	8.6999 mL	17.3998 mL
5 mM	0.3480 mL	1.7400 mL	3.4800 mL
10 mM	0.1740 mL	0.8700 mL	1.7400 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (3.62 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.62 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (3.62 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.62 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.62 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.62 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95.

[2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273.

[3]. Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892.

[4]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004.

[5]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.

Cell Assay ^[3]	The viability of the mouse ES cells is determined after exposure to different concentrations of GSK3 inhibitors for three days using the MTT assay. The decrease of MTT activity is a reliable metabolism-based test for quantifying cell viability; this decrease correlates with the loss of cell viability. 2,000 cells are seeded overnight on gelatine-coated 96-well plates in LIF-containing ES cell medium. On the next day the medium is changed to medium devoid of LIF and with reduced serum and supplemented with 0.1-1 μM BIO, or 1-10 μM SB-216763, CHIR-99021 or CHIR-98014. Basal medium without GSK3 inhibitors or DMSO is used as control. All tested conditions are analyzed in triplicates^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]^[4]	Rats^[1] Primary hepatocytes from male Sprague Dawley rats that weighed <140 g are prepared and used 1-3 h after isolation. aliquots of 1×10⁶cells in 1 mL of DMEM/F12 medium plus 0.2% BSA and CHIR-99021(orally at 16 or 48 mg/kg) or controls are incubated in 12-well plates on a low-speed shaker for 30 min at 37°C in a CO₂-enriched atmosphere, collected by centrifugation and lysed by freeze/thaw in buffer A plus 0.01% NP40; the GS assay is again performed. Mice^[4] Mice 6-10 weeks old are used. The PUMA^+/+ and PUMA^-/- littermates on C57BL/6 background (F10) and Lgr5-EGFP (Lgr5-EGFP-IRES-creERT2) mice are subjected to whole body irradiation (TBI), or abdominal irradiation (ABI). Mice are injected intraperitoneally (i.p.) with 2 mg/kg of CHIR99021 4 h before radiation or 1 mg/kg of SB415286 28 h and 4 h before radiation. Mice are sacrificed to collect small intestines for histology analysis and western blotting. All mice are injected i.p. with 100 mg/kg of BrdU before sacrifice. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Ring DB, et al. Selective glycogen synthase kinase 3 inhibitors potentiate insulin activation of glucose transport and utilization in vitro and in vivo. Diabetes. 2003 Mar;52(3):588-95. [2]. Naujok O, et al. Cytotoxicity and activation of the Wnt/beta-catenin pathway in mouse embryonic stem cells treated with four GSK3 inhibitors.BMC Res Notes. 2014 Apr 29;7:273. [3]. Ye S, et al. Pleiotropy of glycogen synthase kinase-3 inhibition by CHIR99021 promotes self-renewal of embryonic stem cells from refractory mouse strains. PLoS One. 2012;7(4):e35892. [4]. Bennett CN, et al. Regulation of Wnt signaling during adipogenesis. J Biol Chem. 2002 Aug 23;277(34):30998-1004. [5]. Wang X, et al. Pharmacologically blocking p53-dependent apoptosis protects intestinal stem cells and mice from radiation. Sci Rep. 2015 Apr 10;5:8566.

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Volasertib trihydrochloride(Synonyms: 伏拉塞替三盐酸盐; BI 6727 trihydrochloride)

发表于2024年9月10日由上海金畔生物科技有限公司

Volasertib trihydrochloride (Synonyms: 伏拉塞替三盐酸盐; BI 6727 trihydrochloride)

Volasertib (BI 6727) trihydrochloride 是一种具有口服活性的、高效的、ATP 竞争性的 Polo 样激酶 1 (PLK1) 抑制剂，IC₅₀ 为 0.87 nM。Volasertib trihydrochloride 抑制 PLK2 和 PLK3，IC₅₀ 分别为 5 和 56 nM。Volasertib trihydrochloride 诱导有丝分裂停滞和细胞凋亡。Volasertib trihydrochloride 是一种二氢蝶呤酮衍生物，在多种癌症模型中显示出显着的抗肿瘤活性。

Volasertib trihydrochloride Chemical Structure

CAS No. : 946161-17-7

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Volasertib trihydrochloride 的其他形式现货产品:

Volasertib

生物活性

Volasertib (BI 6727) trihydrochloride is an orally active, highly potent and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with an IC₅₀ of 0.87 nM. Volasertib trihydrochloride inhibits PLK2 and PLK3 with IC₅₀s of 5 and 56 nM, respectively. Volasertib trihydrochloride induces mitotic arrest and apoptosis. Volasertib trihydrochloride, a dihydropteridinone derivative, shows marked antitumor activity in multiple cancer models^[1]^[2].

体外研究
(In Vitro)

Volasertib trihydrochloride (BI 6727 trihydrochloride; 0.01-10000 nM; 72 hours) has EC₅₀ values of 11 to 37 nmol/L in multiple cell lines^[1].
Volasertib trihydrochloride (10-1000 nM; 24 hours) results accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase^[1].
Volasertib trihydrochloride (100 nM; 24-72 hours) induces cell apoptosis at 48 hours^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	Multiple cell lines
Concentration:	0.01-10000 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of multiple cell lines derived from various cancer tissues, including carcinomas of the colon (HCT 116, EC₅₀=23 nmol/L) and lung (NCI-H460, EC₅₀=21 nmol/L), melanoma (BRO, EC₅₀=11 nmol/L), and hematopoietic cancers (GRANTA-519, EC₅₀=15 nmol/L; HL-60, EC₅₀=32 nmol/L; THP-1, E₅₀=36 nmol/L and Raji, EC₅₀=37 nmol/L) with EC₅₀ values of 11 to 37 nmol/L.

Apoptosis Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	100 nM
Incubation Time:	24, 48, 72 hours
Result:	G2-M arrest at 24 hours was followed by induction of apoptosis at 48 hours.

Cell Cycle Analysis^[1]

Cell Line:	NCI-H460 cells
Concentration:	10, 30, 100, 300, 1000 nM
Incubation Time:	24 hours
Result:	Resulted in accumulation of cells with 4N DNA content, indicative of a cell cycle block in G2-M phase.

体内研究
(In Vivo)

Volasertib trihydrochloride (BI 6727 trihydrochloride; A total weekly dose of 50 mg/kg; Oral; once a week, twice a week, or daily; for 40 days) shows comparable efficacy in human colon carcinoma xenograft models^[1].
Volasertib trihydrochloride (15, 20, or 25 mg/kg/day; i.v.; 2 consecutive days per week; for 40 days) leads to significant tumor growth delay and even tumor regression in human colon carcinoma xenograft models ^[1].
Volasertib trihydrochloride (70 mg/kg given once weekly or 10 mg/kg daily; oral) significantly delays tumor growth in a non-small cell lung carcinoma xenograft model derived from NCI-H460 cells^[1].
Volasertib (a single dose of 40 mg/kg; iv) causes a significant (13-fold) increase in mitotic cells in HCT 116 tumor-bearing nude mice^[1].
Volasertib has high volume of distribution and a long terminal half-life in mice (V_ss=7.6 L/kg, t_1/2=46 h) and rats (V_ss=22 L/kg, t_1/2=54 h)^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice (Taconic) were grafted s.c. with HCT 116 human colon carcinoma cells (ATCC CCL-247)^[1]
Dosage:	A total weekly dose of 50 mg/kg
Administration:	Oral; once a week, twice a week, or daily; for 40 days
Result:	Showed comparable efficacy and were well tolerated.

Animal Model:	Female BomTac:NMRI-Foxn1^nu mice and male Wistar rats of the strain Crl:WI^[1]
Dosage:	35 mg/kg (mice) or 10 mg/kg (rat) (Pharmacokinetic Analysis)
Administration:	IV 5-minute infusion; a single dose 5-minute infusion
Result:	Had high volume of distribution and a long terminal half-life in mice (V_ss=7.6 L/kg, t_1/2=46 h) and rats (V_ss=22 L/kg, t_1/2=54 h).

Clinical Trial

分子量

728.20

Formula

C₃₄H₅₃Cl₃N₈O₃

CAS 号

946161-17-7

中文名称

伏拉塞替三盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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Braco-19 trihydrochloride

发表于2024年9月8日由上海金畔生物科技有限公司

Braco-19 trihydrochloride 纯度: 98.98%

Braco-19 trihydrochloride 是一种有效的端粒酶/端粒 (telomerase/telomere) 抑制剂，可防止端粒酶的催化作用。Braco-19 trihydrochloride 作为四联体 (GQ) 结合配体，稳定 GQ 四联体在 3V 端粒 DNA 处的形成，并可以导致快速衰老或选择性细胞死亡。Braco-19 trihydrochloride 也是一种HAdV病毒复制抑制剂。

Braco-19 trihydrochloride Chemical Structure

CAS No. : 1177798-88-7

规格	价格	是否有货
1 mg	￥1850	In-stock
5 mg		询价
10 mg		询价

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Braco-19 trihydrochloride 相关产品

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生物活性

Braco-19 trihydrochloride is a potent telomerase/telomere inhibitor, preventing the capping and catalytic action of telomerase. Braco-19 acts as G-quadruplex (GQ) binding ligand, stabilizing G-quadruplexes formation at the 3V telomeric DNA overhang and produce rapid senescence or selective cell death. Braco-19 is also a HAdV virus replication inhibitor^[1]^[2].

IC₅₀ & Target

IC50: telomerase^[1]

体外研究
(In Vitro)

Braco-19 trihydrochloride, as a well-known GQ binding ligand, interacts specifically with the HAdV GQs and increases their stability, and blocks the HAdV multiplication^[2].
BRACO-19 trihydrochloride (1.0-10 μM; 5 day) cause zero growth inhibition is found 1 μM, the IC₅₀ for BRACO-19 in UXF1138L cells is 2.5 μM, the IC₁₀₀ is 5 μM^[1].
BRACO-19 trihydrochloride (1 μM; 24 hours) shows dramatically reduced nuclear hTERT expression. However, residual cytoplasmic hTERT staining is observed accompanied by the occurrence of atypical mitoses^[1].
BRACO-19 trihydrochloride (0-40 μM; 24 hours) decreases the AdV virus growth in a dose-dependent manner in eGFP-transinfected HEK 293 cells^[2].
BRACO-19 trihydrochloride (0-150 μM; 24 hours) shows a decrease in band intensity in an increasing concentration-dependent manner^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[1]

Cell Line:	HEK 293 cells
Concentration:	20 μM; 40 μM
Incubation Time:	24 hours
Result:	Displayed low cytotoxicity and decreased the eGFP fluorescence.

体内研究
(In Vivo)

BRACO-19 trihydrochloride (oral administration or intraperitoneal injection; 2 or 5 mg/kg; 3 weeks) oral dosing regimen are always inactive and the animals have to be sacrificed due to high tumor burden before overall termination of the study, Chronic, i.p. BRACO-19 administration, qdx5 is efficient in inhibiting tumor growth in earlystage xenografts but not advanced-stage xenografts^[1].
BRACO-19 trihydrochloride (intraperitoneal injection; 2 mg/kg; 3 weeks; starting 6 days after transplantation of UXF1138LX fragments) inhibits tumor growth significantly and under these conditions, marked single-agent antitumor activity is observed, with some animals in the group showing complete regressions (5 of 12 tumors)^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Established UXF1138LX Xenografts in nude mice^[1]
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; 3 weeks; starting 6 days after transplantation of UXF1138LX fragments
Result:	Showed partial tumor regressions with an optimal T/C on day 28 of 4.1%, equal to 95.9% inhibition of tumor growth compared with control.

分子量

703.14

Formula

C₃₅H₄₆Cl₃N₇O₂

CAS 号

1177798-88-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : 22 mg/mL (31.29 mM; Need ultrasonic and warming)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.4222 mL	7.1110 mL	14.2219 mL
5 mM	0.2844 mL	1.4222 mL	2.8444 mL
10 mM	0.1422 mL	0.7111 mL	1.4222 mL

参考文献

[1]. Angelika M Burger, et al. The G-quadruplex-interactive Molecule BRACO-19 Inhibits Tumor Growth, Consistent With Telomere Targeting and Interference With Telomerase Function. Cancer Res. 2005 Feb 15;65(4):1489-96.

[2]. Prativa Majee, et al. Genome-wide Analysis Reveals a Regulatory Role for G-quadruplexes During Adenovirus Multiplication. Virus Res. . 2020 Jul 2;283:197960.

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ATM-3507 trihydrochloride

发表于2024年8月31日由上海金畔生物科技有限公司

ATM-3507 trihydrochloride 纯度: 98.10%

ATM-3507 trihydrochloride 是原肌球蛋白 (tropomyosin) 的一个有效抑制剂，其在人类黑色素瘤细胞系中的 IC₅₀ 值约为 3.83-6.84 μM。

ATM-3507 trihydrochloride Chemical Structure

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Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2142	In-stock
5 mg	￥1350	In-stock
10 mg	￥2300	In-stock
50 mg	￥7000	In-stock
100 mg	￥12000	In-stock
200 mg		询价
500 mg		询价

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ATM-3507 trihydrochloride 相关产品

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生物活性

ATM-3507 trihydrochloride is a potent tropomyosin inhibitor with IC₅₀s from 3.83-6.84 μM in human melanoma cell lines.

IC₅₀ & Target

IC50: 3.83-6.84 μM (tropomyosin, in human melanoma celllines)^[1].

体内研究
(In Vivo)

The maximal tolerance dose (MTD) for TR100 and ATM-3507 is 60 and 150 mg/kg, respectively. It is found that a significant inhibition of tumor growth and prolongation of animal survival using either combination compared with each monotherapy. The median survival of mice increased from 18 days for mice treated with ATM-3507 to more than 49 days for mice treated with the combination. It is also found that twice weekly intravenous administration of ATM-3507 also show combination efficacy. The impact of each treatment or the combination on body weight is minimal. Drug levels are measured following the intravenous administration of ATM-3507 at 30 mg/kg in Balb/c mice (n=3 per time point). The mean half-life of ATM-3507 is 5.01 hrs for the terminal elimination phase. The mean AUC_0-t in the plasma is 14,548 ng/h/mL. The C_max of ATM-3507 is 5,758 ng/mL and the the t_1/2 is 5.01 h. The observed plasma clearance and volume of distribution at steady state of ATM-3507 is 33.8 mL/min/kg and 7.23 L/kg, respectively^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

721.17

Formula

C₃₇H₄₉Cl₃FN₅O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (346.66 mM; Need ultrasonic)

H₂O : 33.33 mg/mL (46.22 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3866 mL	6.9332 mL	13.8664 mL
5 mM	0.2773 mL	1.3866 mL	2.7733 mL
10 mM	0.1387 mL	0.6933 mL	1.3866 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline

Solubility: ≥ 2.08 mg/mL (2.88 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (2.88 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (2.88 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Currier MA, et al. Identification of Cancer-Targeted Tropomyosin Inhibitors and Their Synergy with Microtubule Drugs.Mol Cancer Ther. 2017 Aug;16(8):1555-1565.

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A 419259 trihydrochloride(Synonyms: RK 20449 trihydrochloride)

发表于2024年8月9日由上海金畔生物科技有限公司

A 419259 trihydrochloride (Synonyms: RK 20449 trihydrochloride) 纯度: 99.21%

A 419259 trihydrochloride是Src家族激酶抑制剂，对 Src，Lck 和Lyn 的 IC₅₀ 分别为9 nM，3 nM，3 nM。

A 419259 trihydrochloride Chemical Structure

CAS No. : 1435934-25-0

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10 mM * 1 mL in Water	￥1693	In-stock
5 mg	￥1300	In-stock
10 mg	￥1814	In-stock
50 mg	￥6300	In-stock
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A 419259 trihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library

生物活性

A 419259 trihydrochloride is a Src family kinases inhibitor with IC₅₀s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.

IC₅₀ & Target

IC50: 9 nM (Src), <3 nm (lck), <3 (lyn), 3 μm (abl)^[1]

体外研究
(In Vitro)

A 419259 Trihydrochloride is a second-generation pyrrolo-pyrimidine designed to enhance selectivity towards the Src family relative to other cytoplasmic tyrosine kinases. A-419259 inhibits K-562 cells with an IC₅₀ between 0.1 and 0.3 μM, and Meg-01 proliferation with an IC₅₀ of approximately 0.1 μM. A-419259 also potently induces apoptosis in K-562 cells beginning at 0.1 μM and increasing in a dose-dependent manner. PP2 inhibits Src kinase autophosphorylation in both Ph⁺ cell lines (K-562 and Meg-01) with an IC₅₀ between 3 and 10 μM, while A-419259 blocks kinase activation between 0.1 and 0.3 μM. A-419259 strongly inhibits DAGM/Bcr-Abl cell proliferation in the absence of IL-3 with an IC₅₀ between 0.1 and 0.3 μM^[1]. A-419259 is a broad-spectrum pyrrolo-pyrimidine inhibitor, and blocks proliferation and induces apoptosis in CML cell lines. A-419259 inhibits overall SFK activity in K562 and other CML cell lines with an IC₅₀ value of 0.1-0.3 μM^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

592.00

Formula

C₂₉H₃₇Cl₃N₆O

CAS 号

1435934-25-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

H₂O : ≥ 55 mg/mL (92.91 mM)

DMSO : 1 mg/mL (1.69 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6892 mL	8.4459 mL	16.8919 mL
5 mM	0.3378 mL	1.6892 mL	3.3784 mL
10 mM	0.1689 mL	0.8446 mL	1.6892 mL

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

1.

请依序添加每种溶剂： PBS

Solubility: 100 mg/mL (168.92 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88.

[2]. Pene-Dumitrescu T, et al. An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259.Oncogene (2008) 27, 7055-7069

Kinase Assay ^[1]	In vitro kinase assays are performed on His₍₆₎-tagged Lck (residues 62-509) and full-length c-Abl purified from Sf-9 cells, and commercial sources of Lyn, Src and PKC. Lck, Lyn, Src and Abl activities are measured with an ELISA-based assay. Flat bottom 96-well ELISA plates are incubated with a 200 μg/mL solution of Poly(Glu,Tyr) 4 : 1 substrate in phosphate buffered saline (PBS) for 1 h at 37°C and then washed with PBS containing 0.1% Tween-20 (PBS-T). Inhibitor dilutions are added to the washed plates already containing the appropriate enzyme in kinase assay buffer (250 mM Mopso, pH 6.75, 10 mM MgCl₂, 2 mM MnCl₂, 2.5 mM DTT, 0.02% BSA, 2 mM Na₃VO₄, 5% DMSO, 5 μM ATP). After incubation at room temperature for 20 min, plates are washed three times with PBS-T and plate-bound phosphotyrosine is detected with an anti-phosphotyrosine-HRP antibody conjugate and subsequent color development with K-Blue reagents. All assays are optimized to use the least amount of enzyme necessary for a reproducible signal-to-noise ratio^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	K-562 cells are grown in RPMI 1640 supplemented with 10% fetal calf serum (FCS), and 50 g/mL Gentamycin. Meg-01 cells are cultured in Vitacell modified RPMI 1640 (ATCC), supplemented with 10% FCS and 50 μg/mL Gentamycin. The human GM-CSF-dependent myeloid leukemia cell line TF-1 is grown in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 1 ng/mL of recombinant human GM-CSF. DAGM murine myeloid leukemia cells are cultured in RPMI 1640 supplemented with 10% FCS, 50 μg/mL Gentamycin, and 0.5 ng/mL recombinant IL-3. Concentrated stock solutions of PP2 (5 mM) and A-419259 (2 mM) are prepared in DMSO and stored at -20°C. Cellular proliferation is measured using the Live/Dead growth assay. This assay employs calcein-AM, a fluorogenic esterase substrate that is taken up by viable cells and hydrolyzed intracellularly, releasing a green fluorescent product. Briefly, 10⁴ cells are plated per well in 96-well plates for each day of a 4-day time course. Various concentrations of PP2, A-419259 or vehicle control are added to the wells (five wells per concentration per day) and the plates are incubated at 37°C. At each time point, one plate is centrifuged at 1500 g for 10 min to pellet the cells. Cells are washed with phosphate buffered saline (PBS), and calcein-AM is added to each well to a final concentration of 1 μM. Plates are incubated in the dark at room temperature for 1 h. The plates are then read at 485/530 nm (excitation/emission) using a SpectraMax Gemini XS fluorescent plate reader and data are analysed with SoftMax Pro software^[1]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wilson MB, et al. Selective pyrrolo-pyrimidine inhibitors reveal a necessary role for Src family kinases in Bcr-Abl signal transduction and oncogenesis. Oncogene. 2002 Nov 21;21(53):8075-88. [2]. Pene-Dumitrescu T, et al. An inhibitor-resistant mutant of Hck protects CML cells against the antiproliferative and apoptotic effects of the broad-spectrum Src family kinase inhibitor A-419259.Oncogene (2008) 27, 7055-7069

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Zosuquidar trihydrochloride(Synonyms: 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride)

发表于2024年8月3日由上海金畔生物科技有限公司

Zosuquidar trihydrochloride (Synonyms: 唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride) 纯度: 99.79%

Zosuquidar (RS 33295-198) trihydrochloride 是 P-糖蛋白 (P-glycoprotein) 抑制剂，K_i 值为 59 nM。

Zosuquidar trihydrochloride Chemical Structure

CAS No. : 167465-36-3

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5 mg	￥1050	In-stock
10 mg	￥1600	In-stock
50 mg	￥5700	In-stock
100 mg	￥9500	In-stock
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500 mg		询价

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Zosuquidar trihydrochloride 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
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生物活性

Zosuquidar (RS 33295-198) trihydrochloride is an inhibitor of P-glycoprotein with a K_i value of 59 nM.

IC₅₀ & Target

Ki: 59nM (P-glycoprotein)^[1].

体外研究
(In Vitro)

Zosuquidar completely or partially restores drug sensitivity in all P-gp-expressing leukemia cell lines and enhances the cytotoxicity of anthracyclines (daunorubicin, idarubicin, mitoxantrone) and gemtuzumab ozogamicin (Mylotarg) in primary AmL blasts with active P-gp. In addition, P-gp inhibition by zosuquidar is found to be more potent than cyclosporine A in cells with highly active P-gp^[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Zosuquidar trihydrochloride is only moderately active as an inhibitor of P-gp at the blood-brain. An oral dose of 25 mg/kg of zosuquidar trihydrochloride increases the brain concentrations by about 2.5-fold at 1 h and 5-fold at 24 h after paclitaxel administrationbarrier^[3]. Zosuquidar enhances the brain uptake of nelfinavir in a dose-dependent manner. Brain tissue/plasma nelfinavir concentration ratios increase from 0.06±0.03 in the absence of zosuquidar administration and 0.09±0.02 between 2 and 6 h after a 2 mg/kg intravenous dose of zosuquidar to 0.85±0.19 after 6h and 1.58±0.67 after 20 mg/kg zosuquidar^[4].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

636.99

Formula

C₃₂H₃₄Cl₃F₂N₃O₂

CAS 号

167465-36-3

中文名称

唑喹达三盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

溶解性数据

In Vitro:

H₂O : 5 mg/mL (7.85 mM; Need ultrasonic)

DMSO : 1 mg/mL (1.57 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5699 mL	7.8494 mL	15.6988 mL
5 mM	0.3140 mL	1.5699 mL	3.1398 mL
10 mM	—	—	—

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

In Vivo:

1.

Zosuquidar is dissolved in 20% ethanol-saline^[5].

参考文献

[1]. Cripe LD, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood.?201

[2]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson’s disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9.

[3]. Tang R, et al. Zosuquidar?restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AmL). BMC Cancer.?2008 Feb 13;8:51.?

[4]. Kemper EM, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004 Feb;53(2):173-8.

[5]. Anderson BD, et al. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats. Drug Metab Dispos. 2006 Apr;34(4):653-9.

Cell Assay ^[2]	Cells are cultured in 96-well plates. Each drug of interest is added at escalating concentrations in the presence or absence of either zosuquidar or CsA. After 48 hour incubation (except Mylotarg, 4 days incubation), 20 μL of MTT is added to each well for a further 4 hour incubation. The purple precipitate is dissolved in 200 μL DMSO, and the optic density (OD) is determined by the multi-well plate reader^[2]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]^[4]	Rats: Female Sprague-Dawley rats are used in the study. Zosuquidar solutions are prepared in 5% mannitol and adjusted to pH ～2.0 with concentrated HCl. Nelfinavir is infused (10 mg/kg/h) for up to 10 h with or without concurrent administration of an intravenous bolus dose of 2, 6, or 20 mg/kg zosuquidar given at 4 h. Brain tissue and plasma are analyzed for both drug concentrations^[4]. Mice: A stock solution of 5 mg/mL of zosuquidar trihydrochloride is prepared in vehicle solution and diluted in sterile saline. The vehicle solution consisted of 20 g/l mannitol and 1.5 g/l of glycine in water for injection and adjusted to a pH of 2.7 with hydrochloric acid. P-gp knockout mice and wild type mice are used as a model for complete inhibition of P-gp. Zosuquidar trihydrochloride is administered orally at 25 and 80 mg/kg 1 h before i.v. paclitaxel and i.v. at 20 mg/kg 10 min and 1 h before paclitaxel. The concentrations of paclitaxel in plasma and tissues and of zosuquidar trihydrochloride in plasma are quantified by high-performance liquid chromatography^[3]. 上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Cripe LD, et al. Zosuquidar, a novel modulator of P-glycoprotein, does not improve the outcome of older patients with newly diagnosed acute myeloid leukemia: a randomized, placebo-controlled trial of the Eastern Cooperative Oncology Group 3999. Blood.?201 [2]. Hou J, et al. Quantitative determination and pharmacokinetic study of the novel anti-Parkinson’s disease candidate drug FLZ in rat brain by high performance liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2012 Jul;66:232-9. [3]. Tang R, et al. Zosuquidar?restores drug sensitivity in P-glycoprotein expressing acute myeloid leukemia (AmL). BMC Cancer.?2008 Feb 13;8:51.? [4]. Kemper EM, et al. The influence of the P-glycoprotein inhibitor zosuquidar trihydrochloride (LY335979) on the brain penetration of paclitaxel in mice. Cancer Chemother Pharmacol. 2004 Feb;53(2):173-8. [5]. Anderson BD, et al. Dependence of nelfinavir brain uptake on dose and tissue concentrations of the selective P-glycoprotein inhibitor zosuquidar in rats. Drug Metab Dispos. 2006 Apr;34(4):653-9.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

OTS186935 trihydrochloride

发表于2024年8月3日由上海金畔生物科技有限公司

OTS186935 trihydrochloride

OTS186935 trihydrochloride 是一种有效的蛋白甲基转移酶 SUV39H2 抑制剂，IC₅₀ 值为 6.49 nM。OTS186935 trihydrochloride 对小鼠异种移植模型的肿瘤生长有明显的抑制作用，且无明显毒性。OTS186935 trihydrochloride 调节癌细胞中 γ-H2AX 的产生。

OTS186935 trihydrochloride Chemical Structure

CAS No. : 2093401-85-3

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250 mg		询价
500 mg		询价

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OTS186935 trihydrochloride 的其他形式现货产品:

OTS186935 hydrochloride

生物活性

OTS186935 trihydrochloride is a protein methyltransferase SUV39H2 inhibitor with an IC₅₀ of 6.49 nM. OTS186935 trihydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS186935 trihydrochloride regulates the production of γ-H2AX in cancer cells^[1].

IC₅₀ & Target

IC50: 6.49 nM (SUV39H2)^[1]

体外研究
(In Vitro)

OTS186935 trihydrochloride inhibits A549 cell growth with IC₅₀ of 0.67 μM^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

OTS186935 trihydrochloride (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )^[1]
Dosage:	10 mg/kg
Administration:	Intravenously; once daily for 14 days
Result:	Tumor growth inhibition of 42.6% on day 14.

Animal Model:	Female BALB/cAJcl-nu/nu mice (bearing A549 cells)^[1]
Dosage:	25 mg/kg
Administration:	Intravenously; once daily for 14 days
Result:	Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.

分子量

573.34

Formula

C₂₅H₂₉Cl₄N₅O₂

CAS 号

2093401-85-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Vougiouklakis T, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831.

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NVP-BSK805 trihydrochloride

发表于2024年7月10日由上海金畔生物科技有限公司

NVP-BSK805 trihydrochloride

NVP-BSK805 trihydrochloride 是一种 ATP 竞争性的 JAK2 抑制剂，对 JAK2 JH1 (JAK 同源 1)，JAK1 JH1，JAK3 JH1，和 TYK2 JH1 的 IC₅₀ 值分别为 0.48 nM，31.63 nM，18.68 nM 和 10.76 nM。

NVP-BSK805 trihydrochloride Chemical Structure

CAS No. : 2320258-95-3

规格		是否有货
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250 mg		询价
500 mg		询价

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NVP-BSK805 trihydrochloride 的其他形式现货产品:

NVP-BSK805 dihydrochloride

生物活性

NVP-BSK805 trihydrochloride trihydrochloride is an ATP-competitive JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively^[1].

IC₅₀ & Target^[1]

JAK2 JH1

0.48 nM (IC₅₀)

JAK2(V617F)

0.56 nM (IC₅₀)

FL JAK2 wt

0.58 nM (IC₅₀)

TYK2 JH1

18.68 nM (IC₅₀)

JAK1 JH1

31.68 nM (IC₅₀)

体外研究
(In Vitro)

NVP-BSK805 trihydrochloride (BSK 805) is a JAK2 inhibitor, with IC₅₀s of 0.48 nM, 31.63 nM, 18.68 nM, and 10.76 nM for JAK2 JH1 (JAK homology 1), JAK1 JH1, JAK3 JH1, and TYK2 JH1, respectively. NVP-BSK805 trihydrochloride inhibits the full-length wild-type JAK2 (FL JAK2 wt) and FL JAK2 V617F activity, with IC₅₀s of 0.58 ± 0.03 and 0.56 ± 0.04 nM. NVP-BSK805 trihydrochloride is ATP-competitive, with aclculated K_i of 0.43 ± 0.02 nM. NVP-BSK805 trihydrochloride suppresses the growth of JAK2^V617F-bearing acute myeloid leukemia cell lines with GI₅₀ of <100 nm. nvp-bsk805 trihydrochloride blocks the stat5 phosphorylation at ≥100 nm concentrations, and shows a bias for jak2 over jak1 jak3 inhibition in jak2^V617F-mutant cell lines^[1].
NVP-BSK805 trihydrochloride (5 μM) improves P-gp inhibitory activity. NVP-BSK805 trihydrochloride increases sensitization of drug-resistant KBV20C cancer cells to VIC treatment at 10 μM, and such an effect is more effective than a 5 μM dose^[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

NVP-BSK805 trihydrochloride (BSK 805; 150 mg/kg, p.o.) blocks STAT5 phosphorylation, splenomegaly, and leukemic cell spreading in a Ba/F3 JAK2^V617F cell-driven mouse model^[1].
NVP-BSK805 trihydrochloride (50, 75, and 100 mg/kg, p.o.) also suppresses rhEpo-mediated polycythemia and splenomegaly in BALB/c mice^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

599.93

Formula

C₂₇H₃₁Cl₃F₂N₆O

CAS 号

2320258-95-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[1]. Baffert F, et al. Potent and selective inhibition of polycythemia by the quinoxaline JAK2 inhibitor NVP-BSK805. Mol Cancer Ther. 2010 Jul;9(7):1945-55.

[2]. [2].Cheon JH, et al. The JAK2 inhibitors CEP-33779 and NVP-BSK805 have high P-gp inhibitory activity and sensitize drug-resistant cancer cells to vincristine. Biochem Biophys Res Commun. 2017 Sep 2;490(4):1176-1182.

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MS31 trihydrochloride

发表于2024年7月8日由上海金畔生物科技有限公司

MS31 trihydrochloride 纯度: ≥98.0%

MS31 trihydrochloride 是一种高亲和性和选择性的，片段样的甲基赖氨酸读写蛋白 spindlin 1 (SPIN1) 抑制剂，有效破坏 SPIN1 与 H3K4me3 蛋白互相作用 (IC₅₀=77 nM，AlphaLISA；243 nM，FP)。MS31 trihydrochloride 选择性结合 SPIN1 的 Tudor 结构域 II (K_d=91 nM)。MS31 trihydrochloride 能有效抑制含三甲基赖氨酸肽与 SPIN1 的结合，对非肿瘤性细胞无毒。

MS31 trihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4950	In-stock
5 mg	￥4500	In-stock
10 mg	￥6500	In-stock
50 mg	￥16500	In-stock
100 mg	￥22500	In-stock
200 mg		询价
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MS31 trihydrochloride 相关产品

•相关化合物库:

Natural Product Like Compound Library
Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Targeted Diversity Library

生物活性

MS31 trihydrochloride is a potent, highly affinity and selective fragment-like methyllysine reader protein spindlin 1 (SPIN1) inhibitor. MS31 trihydrochloride potently inhibits the interactions between SPIN1 and H3K4me3 (IC₅₀=77 nM, AlphaLISA; 243 nM, FP). MS31 trihydrochloride selectively binds Tudor domain II of SPIN1 (K_d=91 nM). MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, and is not toxic to nontumorigenic cells^[1].

IC₅₀ & Target

IC50: 77 nM (SPIN1 by AlphaLISA), 243 nM (SPIN1 by FP)^[1]
Kd: 91 nM (SPIN1)^[1]

体外研究
(In Vitro)

MS31 trihydrochloride potently inhibits binding of trimethyllysine-containing peptides to SPIN1, displays high binding affinity, is highly selective for SPIN1 over other epigenetic readers and writers, directly engages SPIN1 in cells, and is not toxic to nontumorigenic cells. MS31 trihydrochloride selectively binds tudor domain II of SPIN1^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

450.83

Formula

C₂₀H₃₀Cl₃N₃O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (138.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2181 mL	11.0907 mL	22.1813 mL
5 mM	0.4436 mL	2.2181 mL	4.4363 mL
10 mM	0.2218 mL	1.1091 mL	2.2181 mL

参考文献

[1]. Xiong Y, et al. Discovery of a Potent and Selective Fragment-like Inhibitor of Methyllysine Reader Protein Spindlin 1(SPIN1). J Med Chem. 2019 Jul 24.

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