Vatalanib-d4 dihydrochloride(Synonyms: 瓦他拉尼二盐酸盐 d4 (双盐酸盐))

发表于2024年4月11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。

Vatalanib-d4 dihydrochloride (Synonyms: 瓦他拉尼二盐酸盐 d4 (双盐酸盐))

Vatalanib-d4 (PTK787-d4) dihydrochloride 是 Vatalanib dihydrochloride 的氘代物。Vatalanib dihydrochloride (PTK787 dihydrochloride) 是VEGFR2/KDR的抑制剂，其IC₅₀值为37nM。

Vatalanib-d4 dihydrochloride Chemical Structure

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生物活性	Vatalanib-d4 (PTK787-d4) dihydrochloride is the deuterium labeled Vatalanib dihydrochloride. Vatalanib (PTK787) dihydrochloride is an inhibitor of VEGFR2/KDR with IC₅₀ of 37 nM^[1]^[2].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	423.76
Formula	C₂₀H₁₃D₄Cl₃N₄
中文名称	瓦他拉尼二盐酸盐 d4 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Wood JM, et al. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res. 2000, 60(8 [3]. Wan J, et al. Local recurrence of small cell lung cancer following radiofrequency ablation is induced by HIF-1α expression in the transition zone. Oncol Rep. 2016 Mar;35(3):1297-308. [4]. Murakami M, et al. Tyrosine kinase inhibitor PTK/ZK enhances the antitumor effects of interferon-α/5-fluorouracil therapy for hepatocellular carcinoma cells. Ann Surg Oncol. 2011, 18(2), 589-596.

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Inolitazone dihydrochloride(Synonyms: Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride)

发表于2024年4月11日由上海金畔生物科技有限公司

Inolitazone dihydrochloride (Synonyms: Efatutazone dihydrochloride; CS-7017 dihydrochloride; RS5444 dihydrochloride) 纯度: 98.36%

Inolitazone dihydrochloride (Efatutazone dihydrochloride) 是一种高亲和力的 PPARγ 激动剂，活性依赖于 PPARγ，抑制生长，IC₅₀ 为 0.8 nM。

Inolitazone dihydrochloride Chemical Structure

CAS No. : 223132-38-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4215	In-stock
2 mg	￥2219	In-stock
5 mg	￥3329	In-stock
10 mg		询价
50 mg		询价

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生物活性

Inolitazone dihydrochloride (Efatutazone dihydrochloride) is a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC₅₀ of 0.8 nM for growth inhibition.

IC₅₀ & Target

PPARγ

体外研究
(In Vitro)

Inolitazone dihydrochloride (Efatutazone dihydrochloride) upregulates the cell cycle kinase inhibitor, p21^WAF1/CIP1. Silencing p21^WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM dose of Inolitazone activates PPARγ:RXRα-dependent transcription as demonstrated in a transient transfection assay utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). DRO cells are treated in culture with Inolitazone, Rosiglitazone, or Troglitazone at the indicated concentrations. DRO cells are transiently transfected with PPRE3-tk-luc to examine effective concentrations at which EC₅₀ occurs. The EC₅₀s are 1 nM (Inolitazone), 65 nM (Rosiglitazone) and 631 nM (Troglitazone). Similarly, the calculated inhibitory concentration at IC₅₀ is 0.8 nM for Inolitazone, 75 nM for Rosiglitazone, and 1412 nM for Troglitazone. Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Exposure of 10 nM Inolitazone following transient transfection with the appropriate PPAR isoform (γ, α, or δ) and PPAR response element linked to a luciferase reporter in RIE rat small intestinal cell line, which does not express PPARs, yields increased luciferase activity only in the presence of PPARγ and PPRE3-tk-luc^[1].
DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism^[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)

Inolitazone dihydrochloride (Efatutazone dihydrochloride) plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth. When Inolitazone is administered in the diet to athymic nude mice prior to DRO tumor cell implantation, tumor growth is inhibited in a dose responsive fashion. At the highest dose, 0.025% Inolitazone inhibits growth on day 32 by 94.4% as compared to that of control. In this treatment group, five of 10 animals do not develop demonstrable tumors. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% compared to that of control on day 32 while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Tumors is nest allowed to establish in the mouse and began 0.025% Inolitazone treatment of mice 1 week after DRO or ARO tumor cell implantation. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors as compared to that of their respective controls on day 35^[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.

Clinical Trial

分子量

575.51

Formula

C₂₇H₂₈Cl₂N₄O₄S

CAS 号

223132-38-5

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 : 25 mg/mL (43.44 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7376 mL	8.6879 mL	17.3759 mL
5 mM	0.3475 mL	1.7376 mL	3.4752 mL
10 mM	0.1738 mL	0.8688 mL	1.7376 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: ≥ 2.5 mg/mL (4.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.34 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 (4.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.34 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 (4.34 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.34 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]. Copland JA, et al. Novel high-affinity PPARgamma agonist alone and in combination with paclitaxel inhibits human anaplastic thyroid carcinoma tumor growth via p21WAF1/CIP1. Oncogene. 2006 Apr 13;25(16):2304-17.

[2]. Marlow LA, et al. Reactivation of suppressed RhoB is a critical step for the inhibition of anaplastic thyroid cancer growth. Cancer Res. 2009 Feb 15;69(4):1536-44.

Cell Assay ^[1]	DRO90-1 (DRO) and ARO81 (ARO) cells are plated in 12-well culture plates in triplicate for each condition at an initial concentration of 2×10⁴ cells/well. After overnight incubation, cells are treated with either Inolitazone, Rosiglitazone, Troglitazone, GW9662, or Paclitaxel diluted in DMSO at concentrations indicated in figure legends. All cells receive identical volumes of DMSO and are exposed to each drug for 6 days with medium and drug changed every 48 h. After 6 days, cells are washed with PBS, trypsinized and counted by Beckman Coulter Counter^[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 Administration ^[1]	Mice^[1] Suspensions of 1×10⁶/0.1 mL DRO or ARO cells in RPMI medium are injected subcutaneously in one flank of 3-4 week athymic female nude mice. Mice are changed to specialized diets either 1 week prior or 1 week after tumor implantation and randomly assigned to experimental or control groups with 10 mice per group. Diets consisted either placebo, 0.00025%, 0.0025%, or 0.025% Inolitazone formulated into the diet. Mice weighed between 20-25 g and consume on average 4 g of food per day. For combinatorial studies either placebo, 10 mg/kg or 15 mg/kg paclitaxel is injected i.p. twice weekly. Tumors are measured every 3-4 days for 35 days with calipers and tumor volumes are calculated by the formula: 0.5236(a×b×c), where a is the shortest diameter, b is the diameter perpendicular to a and c is the diameter height. 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]. Copland JA, et al. Novel high-affinity PPARgamma agonist alone and in combination with paclitaxel inhibits human anaplastic thyroid carcinoma tumor growth via p21WAF1/CIP1. Oncogene. 2006 Apr 13;25(16):2304-17. [2]. Marlow LA, et al. Reactivation of suppressed RhoB is a critical step for the inhibition of anaplastic thyroid cancer growth. Cancer Res. 2009 Feb 15;69(4):1536-44.

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生物活性分子抑制剂MS023 dihydrochloride

发表于2024年4月8日由上海金畔生物科技有限公司

MS023 dihydrochloride 纯度: 99.78%

MS023 dihydrochloride 是一种有效选择性的，具有细胞活性的人 I 型蛋白精氨酸甲基转移酶 (PRMTs) 抑制剂，对 PRMT1，PRMT3，PRMT4，PRMT6 和 PRMT8 的 IC₅₀ 分别为 30，119，83，4 和 5 nM。

MS023 dihydrochloride Chemical Structure

CAS No. : 1992047-64-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥793	In-stock
2 mg	￥760	In-stock
5 mg	￥1000	In-stock
10 mg	￥1800	In-stock
25 mg	￥3300	In-stock
50 mg	￥6100	In-stock
100 mg	￥11000	In-stock
200 mg		询价
500 mg		询价

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Transcription Factor Targeted Library

生物活性

MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC₅₀s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively^[1].

IC₅₀ & Target

IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)^[1]

体外研究
(In Vitro)

MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells^[1].
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 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.

Western Blot Analysis^[1]

Cell Line:	MCF7 and HEK293 cells
Concentration:	1.4, 4, 12, 37, 111, 333, and 1000 nM
Incubation Time:	48 hours for MCF7 cells; 20 hours for HEK293 cells
Result:	Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC₅₀=9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC₅₀=56±7 nM).

体内研究
(In Vivo)

Administration of MS023 (160 mg/kg, i.p) in combination with PKC412 (100 mg/kg, i.g.) blocks MLL-r acute lymphoblastic leukemia (ALL) propagation by inhibiting maintenance of functional MLL-r ALL-initiating cells^[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:	NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells^[2]
Dosage:	160 mg/kg
Administration:	Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result:	Combinatorial treatment extended survival of leukemic mice relative to single treatments.

分子量

360.32

Formula

C₁₇H₂₇Cl₂N₃O

CAS 号

1992047-64-9

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:

DMSO : ≥ 150 mg/mL (416.30 mM)

H₂O : 33.33 mg/mL (92.50 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	2.7753 mL	13.8766 mL	27.7531 mL
5 mM	0.5551 mL	2.7753 mL	5.5506 mL
10 mM	0.2775 mL	1.3877 mL	2.7753 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。

参考文献

[1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81.

[2]. Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268.

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生物活性分子抑制剂MS023 dihydrochloride

发表于2024年4月8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。
MS023 dihydrochloride 纯度: 99.78%

MS023 dihydrochloride Chemical Structure

CAS No. : 1992047-64-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥793	In-stock
2 mg	￥760	In-stock
5 mg	￥1000	In-stock
10 mg	￥1800	In-stock
25 mg	￥3300	In-stock
50 mg	￥6100	In-stock
100 mg	￥11000	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

MS023 dihydrochloride 相关产品

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Epigenetics Compound Library
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Reprogramming Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library

生物活性

IC₅₀ & Target

IC50: 30 nM (PRMT1), 119 nM (PRMT3), 83 nM (PRMT4), 4 nM (PRMT6), 5 nM (PRMT8)^[1]

体外研究
(In Vitro)

MS023 (1-1000 nM; 48 hours) inhibits PRMT1 methyltransferase activity in MCF7 cells^[1].
MS023(1-1000 nM; 20 hours) inhibits PRMT6 methyltransferase activity in HEK293 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.

Western Blot Analysis^[1]

Cell Line:	MCF7 and HEK293 cells
Concentration:	1.4, 4, 12, 37, 111, 333, and 1000 nM
Incubation Time:	48 hours for MCF7 cells; 20 hours for HEK293 cells
Result:	Treatment potently and concentration-dependently reduced cellular levels of H4R3me2a (IC₅₀=9±0.2 nM). Treatment concentration-dependently reduced the H3R2me2a mark (IC₅₀=56±7 nM).

体内研究
(In Vivo)

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:	NOD-scid IL2Rgnull (NSG) mice bearing primary MLL-r ALL cells^[2]
Dosage:	160 mg/kg
Administration:	Intraperitoneal injection; PKC412 (100 mg/kg, i.g.), MS023 (160 mg/kg, i.p), or a combination for 4 weeks
Result:	Combinatorial treatment extended survival of leukemic mice relative to single treatments.

分子量

360.32

Formula

C₁₇H₂₇Cl₂N₃O

CAS 号

1992047-64-9

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:

DMSO : ≥ 150 mg/mL (416.30 mM)

H₂O : 33.33 mg/mL (92.50 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	2.7753 mL	13.8766 mL	27.7531 mL
5 mM	0.5551 mL	2.7753 mL	5.5506 mL
10 mM	0.2775 mL	1.3877 mL	2.7753 mL

参考文献

[1]. Eram MS, et al. A Potent, Selective, and Cell-Active Inhibitor of Human Type I Protein Arginine Methyltransferases. ACS Chem Biol. 2016 Mar 18;11(3):772-81.

[2]. Yinghui Zhu, et al. Targeting PRMT1-mediated FLT3 methylation disrupts maintenance of MLL-rearranged acute lymphoblastic leukemia. Blood. 2019 Oct 10;134(15):1257-1268.

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

生物活性分子抑制剂TH1834 dihydrochloride

发表于2024年4月7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。
TH1834 dihydrochloride 纯度: 99.68%

TH1834 dihydrochloride 是一种特异性的 Tip60 (KAT5) 组蛋白乙酰转移酶抑制剂。TH1834 dihydrochloride 可诱导乳腺癌细胞凋亡并增加 DNA 损伤。TH1834 dihydrochloride 不影响相关组蛋白乙酰转移酶 MOF 的活性。抗癌活性。

TH1834 dihydrochloride Chemical Structure

CAS No. : 2108830-09-5

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2260	In-stock
5 mg	￥1600	In-stock
10 mg	￥2900	In-stock
50 mg	￥11500	In-stock
100 mg	￥20500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

TH1834 dihydrochloride 相关产品

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Apoptosis Compound Library
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Anti-Breast Cancer Compound Library
Targeted Diversity Library

生物活性

TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity^[1].

体外研究
(In Vitro)

TH1834 dihydrochloride (0-500 μM; 1 hour; MCF7 cells) treatment significantly reduces the viability of MCF7 cells^[1].
TH1834 dihydrochloride (0-500 μM; 1 hour; MCF7 cells) treatment highly significant increase in cytotoxicity^[1].
TH1834 dihydrochloride (500 μM; 1 hour; MCF7 cells) treatment induces caspase 3 activation in MCF7 cells^[1].
TH1834 dihydrochloride significantly inhibits Tip60 activity in vitro and treating cells with TH1834 results in apoptosis and increased unrepaired DNA damage in breast cancer^[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 Viability Assay^[1]

Cell Line:	MCF7 cells
Concentration:	0 μM, 0.5 μM, 5 μM, 50 μM and 500 μM
Incubation Time:	1 hour
Result:	Significantly reduced the viability of MCF7 cells.

Cell Cytotoxicity Assay^[1]

Cell Line:	MCF7 cells
Concentration:	0 μM, 0.5 μM, 5 μM, 50 μM and 500 μM
Incubation Time:	1 hour
Result:	Highly significant increase in cytotoxicity at all concentrations used.

Western Blot Analysis^[1]

Cell Line:	MCF7 cells
Concentration:	500 μM
Incubation Time:	1 hour
Result:	Marked caspase 3 activation was observed in MCF7 cells in an independent assay.

分子量

641.63

Formula

C₃₃H₄₂Cl₂N₆O₃

CAS 号

2108830-09-5

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 : 125 mg/mL (194.82 mM; Need ultrasonic)

H₂O : 100 mg/mL (155.85 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5585 mL	7.7927 mL	15.5853 mL
5 mM	0.3117 mL	1.5585 mL	3.1171 mL
10 mM	0.1559 mL	0.7793 mL	1.5585 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 (3.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.24 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 (3.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.24 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 (3.24 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.24 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]. Gao C, et al. Rational design and validation of a Tip60 histone acetyltransferase inhibitor. Sci Rep. 2014 Jun 20;4:5372.

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

生物活性分子抑制剂(S,R,S)-AHPC-Me dihydrochloride(Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride)

发表于2024年4月7日由上海金畔生物科技有限公司

生物活性分子抑制剂特异性抑制剂激动剂化合物库重组蛋白 (S,R,S)-AHPC-Me dihydrochloride (Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride) 纯度: 98.24%

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) 是一种基于 (S,R,S)-AHPC 的，可募集 von Hippel-Lindau (VHL) 蛋白的 VHL 配体。(S,R,S)-AHPC-Me dihydrochloride 可用于合成 ARV-771。ARV-771 是一种基于 VHL E3 连接酶的 BET PROTAC 降解剂。ARV-771 可有效降解去势抵抗性前列腺癌 (CRPC) 细胞中的 BET 蛋白，DC₅₀ <1 nM。

(S,R,S)-AHPC-Me dihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2750	In-stock
100 mg	￥2500	In-stock
500 mg	￥7500	In-stock
1 g	￥12000	In-stock
2 g	￥18000	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

(S,R,S)-AHPC-Me dihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library
Ubiquitination Compound Library

生物活性

(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein^[1]. (S,R,S)-AHPC-Me dihydrochloride can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC₅₀ <1 nm^[2].

IC₅₀ & Target

VHL

分子量

517.51

Formula

C₂₃H₃₄Cl₂N₄O₃S

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 : 100 mg/mL (193.23 mM; Need ultrasonic)

DMSO : 50 mg/mL (96.62 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9323 mL	9.6616 mL	19.3233 mL
5 mM	0.3865 mL	1.9323 mL	3.8647 mL
10 mM	0.1932 mL	0.9662 mL	1.9323 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 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 50.0 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]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

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

生物活性分子抑制剂(S,R,S)-AHPC-Me dihydrochloride(Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride)

发表于2024年4月7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
(S,R,S)-AHPC-Me dihydrochloride (Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride) 纯度: 98.24%

(S,R,S)-AHPC-Me dihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥2750	In-stock
100 mg	￥2500	In-stock
500 mg	￥7500	In-stock
1 g	￥12000	In-stock
2 g	￥18000	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

(S,R,S)-AHPC-Me dihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library
Ubiquitination Compound Library

生物活性

IC₅₀ & Target

VHL

分子量

517.51

Formula

C₂₃H₃₄Cl₂N₄O₃S

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 : 100 mg/mL (193.23 mM; Need ultrasonic)

DMSO : 50 mg/mL (96.62 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9323 mL	9.6616 mL	19.3233 mL
5 mM	0.3865 mL	1.9323 mL	3.8647 mL
10 mM	0.1932 mL	0.9662 mL	1.9323 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 50.0 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: ≥ 5 mg/mL (9.66 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (9.66 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 50.0 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]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

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

Vofopitant dihydrochloride(Synonyms: GR 205171A)

发表于2024年4月7日由上海金畔生物科技有限公司

Vofopitant dihydrochloride (Synonyms: GR 205171A) 纯度: 99.11%

Vofopitant dihydrochloride (GR 205171A) 是一种有效、选择性的，口服有效的速激肽 NK1 受体拮抗剂，在大鼠和人类细胞膜上抑制 [³H]SP 与 NK1 结合的 pK_i 值分别为 9.5 和 10.6，具有成为广谱的止吐剂的潜力。

Vofopitant dihydrochloride Chemical Structure

CAS No. : 168266-51-1

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3890	In-stock
5 mg	￥3500	In-stock
10 mg	￥5500	In-stock
50 mg	￥16500	In-stock
100 mg	￥22500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

Vofopitant dihydrochloride 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
GPCR/G Protein Compound Library
Neuronal Signaling Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Drug Repurposing Compound Library
Endocrinology Compound Library
Neurotransmitter Receptor Compound Library

生物活性

Vofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist, inhibits [³H]SP binding to the NK1 receptor with pK_i values of 9.5 and 10.6 in rat and human membranes respectively, acts as a potential broad-spectrum anti-emetic agent^[1].

IC₅₀ & Target

pKi: 9.5 (NK1, rat), 10.6 (NK1, human)^[1]

Clinical Trial

分子量

505.36

Formula

C₂₁H₂₅Cl₂F₃N₆O

CAS 号

168266-51-1

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 : 33.33 mg/mL (65.95 mM; Need ultrasonic)

DMSO : 33.33 mg/mL (65.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9788 mL	9.8939 mL	19.7879 mL
5 mM	0.3958 mL	1.9788 mL	3.9576 mL
10 mM	0.1979 mL	0.9894 mL	1.9788 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: ≥ 2.5 mg/mL (4.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.95 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 (4.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.95 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 (4.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.95 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]. Gardner CJ, et al. GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity. Regul Pept. 1996 Aug 27;65(1):45-53.

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

生物活性分子抑制剂Ipatasertib dihydrochloride(Synonyms: GDC-0068 dihydrochloride; RG-7440 dihydrochloride)

发表于2024年4月6日由上海金畔生物科技有限公司

生物活性分子抑制剂特异性抑制剂激动剂化合物库重组蛋白 Ipatasertib dihydrochloride (Synonyms: GDC-0068 dihydrochloride; RG-7440 dihydrochloride) 纯度: 99.27%

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) 是一种选择性的，ATP竞争性的 pan-Akt 抑制剂，抑制 Akt1，Akt2，Akt3 的 IC₅₀ 分别为 5，18，8 nM。

Ipatasertib dihydrochloride Chemical Structure

CAS No. : 1396257-94-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1285	In-stock
2 mg	￥650	In-stock
5 mg	￥1100	In-stock
10 mg	￥1600	In-stock
50 mg	￥4300	In-stock
100 mg	￥6000	In-stock
200 mg	￥9000	In-stock
500 mg	￥18000	In-stock
1 g	￥29800	In-stock
5 g		询价
10 g		询价

* Please select Quantity before adding items.

Ipatasertib dihydrochloride 相关产品

•相关化合物库:

Drug Repurposing Compound Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Kinase Inhibitor Library
PI3K/Akt/mTOR Compound Library
Stem Cell Signaling Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Autophagy Compound Library
Anti-Aging Compound Library
Drug Repurposing Compound Library
Differentiation Inducing Compound Library
Oxygen Sensing Compound Library
Glycolysis Compound Library
Cytoskeleton 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
Rare Diseases Drug Library
Anti-Colorectal Cancer Compound Library

生物活性

Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC₅₀s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.

IC₅₀ & Target^[1]

Akt1

5 nM (IC₅₀)

Akt3

8 nM (IC₅₀)

Akt2

18 nM (IC₅₀)

PKA

3100 nM (IC₅₀)

体外研究
(In Vitro)

Ipatasertib shows more than 600 and more than 100-fold selectivity for Akt1 in IC₅₀ against the closely related kinases PKA and p70S6K, respectively. When tested at 1 μM in a panel of 230 protein kinases, which includes 36 human AGC family members, Ipatasertib inhibits only 3 other kinases by more than 70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K). IC₅₀s measured for these 3 kinases are 98, 69, and 860 nM, respectively. Thus, with the exception of PKG1 (relative to which Ipatasertib is >10-fold more selective for Akt1), Ipatasertib displays a more than 100-fold selectivity for Akt1 over the next most potently inhibited non-Akt kinase, p70S6K, in the screening kinase panel. The relationship between pharmacokinetics (PK) and pharmacodynamics (PD) of Ipatasertib is investigated in 3 xenograft models that showed dose-dependent response to drug treatment: MCF7-neo/HER2, TOV-21G.x1, and LNCaP. The mean cell viability IC₅₀ of Ipatasertib in these 3 cell lines is 2.56, 0.44, and 0.11 μM, respectively^[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)

Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone^[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.

Clinical Trial

分子量

530.92

Formula

C₂₄H₃₄Cl₃N₅O₂

CAS 号

1396257-94-5

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 : 125 mg/mL (235.44 mM; Need ultrasonic)

H₂O : ≥ 41 mg/mL (77.22 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	1.8835 mL	9.4176 mL	18.8352 mL
5 mM	0.3767 mL	1.8835 mL	3.7670 mL
10 mM	0.1884 mL	0.9418 mL	1.8835 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： 5% DMSO 40% PEG300 5% Tween-80 50% saline

Solubility: ≥ 3.88 mg/mL (7.31 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)

Solubility: ≥ 3.88 mg/mL (7.31 mM); Clear solution
3.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
4.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
5.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
6.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
7.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
8.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
9.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
10.

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

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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
11.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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。
12.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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。
13.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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。
14.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.08 mg/mL (3.92 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.92 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]. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27.

[2]. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

Cell Assay ^[2]	The 384-well plates are seeded with 2,000 cells per well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO₂ overnight (~16 hours). Compounds (e.g., Ipatasertib) are diluted in DMSO to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments are tested in quadruplicates. After 4 days incubation, relative numbers of viable cells are estimated using CellTiter-Glo and total luminescence is measured on a Wallac Multilabel Reader. The concentration of drug resulting in IC₅₀ is calculated from a 4-parameter curve analysis (XLfit) and is determined from a minimum of 3 experiments. For cell lines that failed to achieve an IC₅₀, the highest concentration tested (10 μM) is listed^[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 ^[2]	Mice^[2] In vivo efficacy is evaluated in multiple tumor cell line- and patient-derived xenograft models. Cells or tumor fragments are implanted subcutaneously into the flank of immunocompromised mice. Female or male nude (nu/nu) or severe combined immunodeficient mice (SCID)/beige mice are used. The LuCaP35V patient-derived primary tumors are obtained; male mice are castrated before implantation of tumor fragments. After implantation of tumor cells or fragments into mice, tumors are monitored until they reached mean tumor volumes of 180 to 350 mm³ and distributed into groups of 8 to 10 animals/group. Ipatasertib is formulated in 0.5% methylcellulose/0.2% Tween-80 (MCT) and administered daily (QD), via oral (per os; PO) gavage. RP-56976 is formulated in 3% EtOH/97% saline and dosed intravenously (IV) every week (QW) at 2.5 or 7.5 mg/kg. NSC 241240 is formulated in saline and dosed intraperitoneally (IP) weekly at 50 mg/kg. 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]. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27;55(18):8110-27. [2]. Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72.

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Meclizine-d8 dihydrochloride(Synonyms: Meclozine-d8 dihydrochloride)

发表于2024年4月5日由上海金畔生物科技有限公司

Meclizine-d8 dihydrochloride (Synonyms: Meclozine-d8 dihydrochloride)

Meclizine-d8 (Meclozine-d8) dihydrochloride 是 Meclizine dihydrochloride 的氘代物。Meclizine (Meclozine) dihydrochloride 是一种抗组胺剂 (antihistamine)，可逆地抑制组胺与 H1 受体的相互作用。Meclizine dihydrochloride 是哌嗪类 H1 拮抗剂。Meclizine dihydrochloride 是一种有效的抗晕车剂。Mecliz

Meclizine-d8 dihydrochloride Chemical Structure

CAS No. : 1432062-16-2

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

* Please select Quantity before adding items.

生物活性	Meclizine-d8 (Meclozine-d8) dihydrochloride is the deuterium labeled Meclizine dihydrochloride. Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington’s disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR^[1]^[2]^[3].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	471.92
Formula	C₂₅H₂₁D₈Cl₃N₂
CAS 号	1432062-16-2
中文名称	盐酸美克洛嗪 d8 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Priti N. Patel, et al. Safety and Efficacy in the Treatment and Prevention of Motion Sickness. [3]. Vishal M Gohil, et al. Meclizine is neuroprotective in models of Huntington’s disease. Hum Mol Genet. 2011 Jan 15;20(2):294-300. [4]. Wendong Huang, et al. Meclizine Is an Agonist Ligand for Mouse Constitutive Androstane Receptor (CAR) and an Inverse Agonist for Human CAR [5]. Seiji Kishi, et al. Meclizine Preconditioning Protects the Kidney Against Ischemia-Reperfusion Injury. EBioMedicine. 2015 Jul 29;2(9):1090-101.

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MPP dihydrochloride

发表于2024年3月21日由上海金畔生物科技有限公司

MPP dihydrochloride 纯度: 98.67%

MPP dihydrochloride 是一种高度选择性的雌激素受体 α (ERα) 拮抗剂。MPP dihydrochloride 降低了 p-ERα/ERα 的比率。

MPP dihydrochloride Chemical Structure

CAS No. : 911295-24-4

规格	价格	是否有货
5 mg	￥1900	In-stock
10 mg	￥3000	In-stock
25 mg	￥9100	询价
50 mg	￥14500	询价
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

MPP dihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Anti-Cancer Compound Library
Anti-Breast Cancer Compound Library

生物活性

MPP dihydrochloride is a highly selective estrogen receptor alpha (ERα) antagonist. MPP dihydrochloride reduces the ratio of p-ERα/ERα^[1].

体外研究
(In Vitro)

MPP (1, 5, 10, 25, 50 and 100 µM; 24 h) decreases cell viability with an IC₅₀ value of 20.01 µM in RL95-2 cells^[1].
MPP dihydrochloride shows antiproliferative activity at a concentration of 10 μM in RL95-2 cells^[1].
MPP dihydrochloride (20 µM; 24 h) reduces the phosphorylation of ERα, while it does not alter the phosphorylation of Akt. MPP dihydrochloride reduces the ratio of p-ERα/ERα^[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 Viability Assay^[1]

Cell Line:	RL95-2 endometrium cancer cells
Concentration:	1, 5, 10, 25, 50 and 100 µM
Incubation Time:	24 hours
Result:	The treatment with 25 µM, 50 µM and 100 µM for 24 h decreased cell viability significantly. However, cell viability was not significantly changed by MPP dihydrochloride at concentration below 25 µM.

Cell Proliferation Assay^[1]

Cell Line:	RL95-2 cell
Concentration:	10, 15, 20 and 25 µM
Incubation Time:	72 hours
Result:	Showed antiproliferative activity at a concentration of 10 μM.

Western Blot Analysis^[1]

Cell Line:	RL95-2 cell line
Concentration:	20 µM
Incubation Time:	24 hours
Result:	Reduced the phosphorylation of ERα, while it did not alter the phosphorylation of Akt. Reduced the ratio of p-ERα/ERα compared to the control group.

体内研究
(In Vivo)

MPP (Low dose 20 μg/kg body weight or high dose 200 μg/kg body weight) leads to a dose-dependent attenuation of percent prepulse inhibition (PPI)^[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:	Male C57BL/6N mice at the age of 9-10 weeks^[2]
Dosage:	Low dose (20 μg/kg body weight) or high dose (200 μg/kg body weight)
Administration:	Administered subcutaneously (s.c.) injected; injection volume of 5 mL/kg; 60 min before PPI testing
Result:	Led to a dose-dependent attenuation of percent PPI. Pretreatment with 200 μg/kg reduced the mean percent PPI scores by ~30%.

分子量

542.50

Formula

C₂₉H₃₃Cl₂N₃O₃

CAS 号

911295-24-4

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)

参考文献

[1]. Karaboğa Arslan AK, et al. α-Chaconine and α-Solanine Inhibit RL95-2 Endometrium Cancer Cell Proliferation by Reducing Expression of Akt (Ser473) and ERα (Ser167). Nutrients. 2018 May 25;10(6). pii: E672.

[2]. Labouesse MA, et al. Effects of selective estrogen receptor alpha and beta modulators on prepulse inhibition in male mice. Psychopharmacology (Berl). 2015 Aug;232(16):2981-94.

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Furamidine dihydrochloride(Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride)

发表于2024年3月20日由上海金畔生物科技有限公司

Furamidine dihydrochloride (Synonyms: DB75 dihydrochloride; NSC 305831 dihydrochloride) 纯度: ≥98.0%

Furamidine dihydrochloride (DB75 dihydrochloride) 是一种选择性的且细胞可渗透的蛋白精氨酸甲基转移酶 1 (PRMT1) 抑制剂，IC₅₀ 为 9.4 μM。Furamidine dihydrochloride 对 PRMT1 的选择性高于 PRMT5，PRMT6 和 PRMT4 (CARM1) (IC₅₀ 分别为 166 µM，283 µM 和 >400 µM)。Furamidine dihydrochloride 是一种有效的，可逆的和竞争性的酪氨酰 DNA 磷酸二酯酶 1 (TDP-1) 抑制剂。Furamidine dihydrochloride 对 TDP-1 的抑制作用对单链和双链 DNA 底物均有效，对双链 DNA 的作用更强。Furamidine dihydrochloride 也是一种抗寄生虫剂。

Furamidine dihydrochloride Chemical Structure

CAS No. : 55368-40-6

规格	价格	是否有货
5 mg	￥3500	In-stock
10 mg		询价
50 mg		询价

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Furamidine dihydrochloride 相关产品

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Bioactive Compound Library Plus
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Immunology/Inflammation Compound Library
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Histone Modification Research Compound Library
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Reprogramming Compound Library
Anti-Alzheimer’s Disease Compound Library
Anti-Blood Cancer Compound Library
Antiparasitic Compound library
Neurodegenerative Disease-related Compound Library
Targeted Diversity Library
Anti-Colorectal Cancer Compound Library

生物活性

Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC₅₀ of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC₅₀s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent^[1]^[2]^[3].

IC₅₀ & Target

IC50: 9.4 μM (Protein arginine methyltransferase 1 (PRMT1)); 166 µM (PRMT5), 283 µM (PRMT6) and >400 µM (PRMT4)^[1]
Parasite^[1]
Tyrosyl-DNA phosphodiesterase 1 (TDP-1)^[2]

体外研究
(In Vitro)

Furamidine (compound 1; 20 μM; 72 hours; leukemia cell lines) inhibits cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations^[1].
Furamidine (compound 1; 20 μM; 15 hours; 293T cells) treatment significantly reduces the expression level of the methylated GFP-ALY protein in 293T cells^[1].
Furamidine binds duplex DNA in the DNA minor groove selectively at AT rich sites [(A/T)4]. Furamidine can also intercalate between GC base pairs of duplex DNA. Furamidine could therefore interfere with DNA processing enzymes such as TDP-1^[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:	Meg-01, K562, HL-60, NB4, MOLM13, HEL, CMK, CMY, CMS and CHRF cells
Concentration:	20 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth for most of the leukemia cell lines except HEL cells which have JAK2V617F mutations.

Western Blot Analysis^[1]

Cell Line:	293T cells
Concentration:	20 μM
Incubation Time:	15 hours
Result:	The expression level of the methylated GFP-ALY protein is significantly reduced.

体内研究
(In Vivo)

Furamidine (1 mg/kg; intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks; female NZB/NZW mice) and Irinotecan combined treatment suppresses proteinuria and prolongs survival of lupus-prone NZB/NZW mice. The combination treatment does not change the levels of anti-dsDNA antibodies^[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 Model:	Female NZB/NZW mice (6-week-old) with Irinotecan (1 mg/kg)^[3]
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection; 3 times a week and repeated every 4 weeks; for 34 weeks
Result:	Suppressed proteinuria and prolongs survival of lupus-prone NZB/NZW mice combined with Irinotecan.

分子量

377.27

Formula

C₁₈H₁₈Cl₂N₄O

CAS 号

55368-40-6

中文名称

呋喃脒二盐酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 12.5 mg/mL (33.13 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6506 mL	13.2531 mL	26.5062 mL
5 mM	0.5301 mL	2.6506 mL	5.3012 mL
10 mM	0.2651 mL	1.3253 mL	2.6506 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: ≥ 1.25 mg/mL (3.31 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.31 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 12.5 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% corn oil

Solubility: ≥ 1.25 mg/mL (3.31 mM); Clear solution

此方案可获得 ≥ 1.25 mg/mL (3.31 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 12.5 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]. Yan L, et al. Diamidine compounds for selective inhibition of protein arginine methyltransferase 1. J Med Chem. 2014 Mar 27;57(6):2611-22.

[2]. Antony S, et al. Novel high-throughput electrochemiluminescent assay for identification of human tyrosyl-DNA phosphodiesterase (Tdp1) inhibitors and characterization of furamidine (NSC 305831) as an inhibitor of Tdp1. Nucleic Acids Res. 2007;35(13):4474-84.

[3]. Keil A, et al. The Topoisomerase I Inhibitor Irinotecan and the Tyrosyl-DNA Phosphodiesterase 1 Inhibitor Furamidine Synergistically Suppress Murine Lupus Nephritis. Arthritis Rheumatol. 2015 Jul;67(7):1858-67.

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Peldesine dihydrochloride(Synonyms: BCX 34 dihydrochloride)

发表于2024年3月20日由上海金畔生物科技有限公司

Peldesine dihydrochloride (Synonyms: BCX 34 dihydrochloride) 纯度: 99.80%

Peldesine (BCX 34) dihydrochloride 是一种有效的，竞争性，可逆和口服活性的嘌呤核苷磷酸化酶 (PNP) 抑制剂，对人，大鼠和小鼠红细胞 (RBC) PNP 的 IC₅₀ 分别为 36 nM，5 nM 和 32 nM。Peldesine dihydrochloride 还是一种 T 细胞 (T-cell) 增殖抑制剂，IC₅₀ 为 800 nM。Peldesine dihydrochloride 可用于皮肤 T 细胞淋巴瘤，牛皮癣和 HIV 感染的研究。

Peldesine dihydrochloride Chemical Structure

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5 mg	￥4200	In-stock
10 mg	￥7000	In-stock
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生物活性

Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC₅₀s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC₅₀ of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research^[1]^[2]^[3]^[4].

IC₅₀ & Target

IC50: 36 nM (Human RBC PNP), 5 nM (Rat RBC PNP), 32 nM (Mouse RBC PNP), and 800 nM (Human T-cell proliferation)^[3]
Ki: 23 nM (Human RBC PNP)^[3]
HIV^[4]

体外研究
(In Vitro)

Peldesine (BCX 34; 0-50 µM; 72 hours; Jurkat cells) could inhibit the T-cell proliferation completely at a concentration of less than 10 μM, in the presence of dGuo (10 μM). In contrast, the B-cell proliferation is not affected by Peldesine^[1].
Peldesine (BCX 34) suppresses T-cell immune reaction in an IL-2-independent manner, and this means that Peldesine might affect a late phase rather than an early stage in T-cell activation^[1].
Peldesine also, in the presence but not in the absence of deoxyguanosine, inhibits human leukemia CCRF-CEM T-cell proliferation with an IC₅₀ of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM^[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.

Cell Viability Assay^[1]

Cell Line:	Jurkat cells
Concentration:	0-50 µM
Incubation Time:	72 hours
Result:	In the presence of 10 µM dCuo, had a complete inhibitory effect for T-cell lines.

Clinical Trial

分子量

314.17

Formula

C₁₂H₁₃Cl₂N₅O

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 : 200 mg/mL (636.60 mM; Need ultrasonic)

H₂O : 33.33 mg/mL (106.09 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1830 mL	15.9150 mL	31.8299 mL
5 mM	0.6366 mL	3.1830 mL	6.3660 mL
10 mM	0.3183 mL	1.5915 mL	3.1830 mL

参考文献

[1]. Wada Y, et al. BCX-34: a novel T-cell selective immunosuppressant: purine nucleoside phosphorylase (PNP) inhibitor. Artif Organs. 1996 Aug;20(8):849-52.

[2]. Duvic M, et al. A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma. J Am Acad Dermatol. 2001 Jun;44(6):940-7.

[3]. Bantia S, et al. In vivo and in vitro pharmacologic activity of the purine nucleoside phosphorylase inhibitor BCX-34: the role of GTP and dGTP. Immunopharmacology. 1996 Oct;35(1):53-63.

[4]. New AIDS study suppresses T cells to stop viral growth. AIDS Alert. 1997 Jul;12(7):77-8.

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Nolatrexed-d4 dihydrochloride(Synonyms: 盐酸诺拉曲塞 d4 (双盐酸盐))

发表于2024年3月19日由上海金畔生物科技有限公司

Nolatrexed-d4 dihydrochloride (Synonyms: 盐酸诺拉曲塞 d4 (双盐酸盐))

Nolatrexed-d4 dihydrochloride 是 Nolatrexed dihydrochloride 的氘代物。Nolatrexed dihydrochloride (AG 337) 是一种非竞争性的胸苷酸合酶 (thymidylate synthase) 抑制剂，与该酶的叶酸辅因子结合位点相互作用，对人 thymidylate synthase 的 K_i 值为 11 nM。Nolatrexed dihydrochloride (AG 337) 能够在癌细胞 S 期诱导细胞周期停滞。具有抗癌活性。

Nolatrexed-d4 dihydrochloride Chemical Structure

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生物活性	Nolatrexed-d4 dihydrochloride (AG 337-d4) is the deuterium labeled Nolatrexed dihydrochloride. Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a K_i of 11 nM for human thymidylate synthase^[1]. Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity^[2].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	361.28
Formula	C₁₄H₁₀D₄Cl₂N₄OS
中文名称	盐酸诺拉曲塞 d4 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Webber S, et al. AG337, a novel lipophilic thymidylate synthase inhibitor: in vitro and in vivo preclinical studies. Cancer Chemother Pharmacol. 1996;37(6):509-17. [3]. McGuire JJ, et al. Characterization of the effect of AG337, a novel lipophilic thymidylate synthase inhibitor, on human head and neck and human leukemia cell lines.

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Ranolazine-d8 dihydrochloride(Synonyms: CVT 303-d8 dihydrochloride; RS 43285-d8)

发表于2024年3月19日由上海金畔生物科技有限公司

Ranolazine-d8 dihydrochloride (Synonyms: CVT 303-d8 dihydrochloride; RS 43285-d8)

Ranolazine-d8 (CVT 303-d8) dihydrochloride 是 Ranolazine dihydrochloride 的氘代物。Ranolazine dihydrochloride (CVT 303 dihydrochloride) 是一种抗心绞痛和抗缺血剂，可通过抑制内向钠电流的后期作用 (对 I_Na 和 I_Kr 的 IC₅₀ 值分别为 6 μM 和 12 μM) 来发挥功效，而不会影响心率或血压。Ranolazine dihydrochloride 还是脂肪酸氧化的部分抑制剂。

Ranolazine-d8 dihydrochloride Chemical Structure

CAS No. : 1219802-60-4

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生物活性	Ranolazine-d8 (CVT 303-d8) dihydrochloride is the deuterium labeled Ranolazine dihydrochloride. Ranolazine dihydrochloride (CVT 303 dihydrochloride) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)^[1]^[2]. Ranolazine dihydrochloride is also a partial fatty acid oxidation inhibitor^[3].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	508.51
Formula	C₂₄H₂₇D₈Cl₂N₃O₄
CAS 号	1219802-60-4
中文名称	盐酸雷诺嗪 d8 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Keating GM. Ranolazine: A Review of Its Use as Add-On Therapy in Patients with Chronic Stable Angina Pectoris. Drugs. 2013 Jan;73(1):55-73. [3]. Wang WQ, Robertson C, Dhalla AK, Belardinelli L. Antitorsadogenic effects of ({+/-})-N-(2,6-dimethyl-phenyl)-(4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits. J Pharmacol Exp Ther. 2008 Jun;325(3):875-81. doi: 10.1124/jpet.108.137729. Epub 2008 Mar 5. [4]. Zacharowski K, Blackburn B, Thiemermann C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur J Pharmacol. 2001 Apr 20;418(1-2):105-10.

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Dacomitinib-d10 dihydrochloride(Synonyms: PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride)

发表于2024年3月18日由上海金畔生物科技有限公司

Dacomitinib-d10 dihydrochloride (Synonyms: PF-00299804-d10 dihydrochloride; PF-299804-d10 dihydrochloride)

Dacomitinib-d10 (PF-00299804-d10) dihydrochloride 是 Dacomitinib dihydrochloride 的氘代物。Dacomitinib (PF-00299804) dihydrochloride 是一种特异，不可逆的 ERBB 家族抑制剂，作用于 EGFR，ERBB2 和 ERBB4 的 IC₅₀ 分别为 6 nM，45.7 nM 和 73.7 nM

Dacomitinib-d10 dihydrochloride Chemical Structure

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生物活性	Dacomitinib-d10 (PF-00299804-d10) dihydrochloride is the deuterium labeled Dacomitinib dihydrochloride. Dacomitinib (PF-00299804) dihydrochloride is a specific and irreversible inhibitor of the ERBB family of kinases with IC₅₀s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	552.92
Formula	C₂₄H₁₇D₁₀Cl₃FN₅O₂
中文名称	达克替尼 d10 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Engelman JA, et al. PF00299804, an irreversible pan-ERBB inhibitor, is effective in lung cancer models with EGFR and ERBB2 mutations that are resistant to ZD1839. Cancer Res. 2007 Dec 15;67(24):11924-32. [3]. Kalous O, et al. Dacomitinib (PF-00299804), an irreversible Pan-HER inhibitor, inhibits proliferation of HER2-amplified breast cancer cell lines resistant to Anti-Human HER2 and GW572016. Mol Cancer Ther. 2012 Sep;11(9):1978-87.

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Lerociclib dihydrochloride(Synonyms: G1T38 dihydrochloride)

发表于2024年3月18日由上海金畔生物科技有限公司

Lerociclib dihydrochloride (Synonyms: G1T38 dihydrochloride) 纯度: 99.74%

Lerociclib dihydrochloride (G1T38 dihydrochloride) 是一种有效的选择性 CDK4/CDK6 抑制剂，抑制 CDK4/CyclinD1 和 CDK6/CyclinD3，IC₅₀ 值分别为 1 nM 和 2 nM。

Lerociclib dihydrochloride Chemical Structure

CAS No. : 2097938-59-3

规格	价格	是否有货
5 mg	￥4800	In-stock
10 mg	￥7500	In-stock
25 mg	￥14500	In-stock
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100 mg		询价

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生物活性

Lerociclib dihydrochloride (G1T38 dihydrochloride) is a potent and selective inhibitor of CDK4/CDK6, with IC₅₀s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

IC₅₀ & Target^[1]

Cdk4/cyclin D1

1 nM (IC₅₀)

cdk6/cyclin D3

2 nM (IC₅₀)

CDK9/Cyclin T

28 nM (IC₅₀)

CDK5/p35

832 nM (IC₅₀)

Cdk5/p25

1.2 μM (IC₅₀)

cdk2/cyclin A

1.5 μM (IC₅₀)

CDK2/cyclinE

3.6 μM (IC₅₀)

CDK1/cyclinB1

2.4 μM (IC₅₀)

CDK7/Cyclin H/MAT1

2.4 μM (IC₅₀)

体外研究
(In Vitro)

Within the CDK family, Lerocyclib is least selective against CDK9/cyclin T, ~30 fold between CDK4/cyclin D1 and CDK9/ cyclin T at the biochemical IC₅₀. Lerociclib produces a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC₅₀ of ~20 nM. A dose dependent increase of cells in the G1 phase of the cell cycle is observed when CDK4/6 dependent WM2664 cells are treated with G1T38 for 24 hours. This arrest is maintained through 300 nM, more than 300x the biochemical IC₅₀. WM2664 cells treated with 30-1000 nM of Lerociclib for 24 hours exhibits a complete inhibition of RB phosphorylation compared to vehicle controls. Treatment with G1T38 reduces RB phosphorylation within 1 hour post-treatment and generates near complete inhibition of RB phosphorylation by 16 hours post-treatment. G1T38 produces a robust inhibition of proliferation in a diverse array of tumor cell lines including breast, melanoma, leukemia and lymphoma with EC₅₀ concentrations as low as 23 nM^[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.

体内研究
(In Vivo)

In this HER2⁺ breast cancer model, Mice treated with Lerociclib elicits 8% tumor regression after 21 days of treatment while control animals have a 577% increase in tumor burden over the same treatment period. Compared to the vehicle-treated mice, daily treatment with 100 mg/kg of Lerociclib or palbociclib shows tumor regression within 10 days in the MCF7 xenograft model. After 27 days of treatment, tumor growth inhibition is observed in the 10, 50, and 100 mg/kg Lerociclib cohorts (approximately 12%, 74%, and 90% inhibition, respectively). Daily oral palbociclib treatment causes an 18%, 66%, and 87% tumor growth inhibition in the 10, 50, and 100 mg/kg dosage cohorts, respectively. Interestingly, at 50 mg/kg, Lerociclib is significantly more efficaciou than palbociclib. Similar results are seen in the ER⁺ ZR-75-1 breast cancer xenograft model when comparing Lerocyclib and palbociclib at the 50 mg/kg dose. Lerociclib treated mice exhibits 77% TGI with an overall 60% tumor growth delay demonstrating Lerociclib alone is highly efficacious in this NSCLC tumor model^[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.

Clinical Trial

分子量

547.52

Formula

C₂₆H₃₆Cl₂N₈O

CAS 号

2097938-59-3

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 : 4 mg/mL (7.31 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8264 mL	9.1321 mL	18.2642 mL
5 mM	0.3653 mL	1.8264 mL	3.6528 mL
10 mM	—	—	—

参考文献

[1]. Bisi JE, et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343-42358.

Cell Assay ^[1]	SupT1, Daudi, MCF7, ZR-75-1, A2058, WM2664, and H69 cells are seeded at 1000 cells per well; MV-4-11 and BV173 cells are plated at 4000 cells per well; Tom-1 cells are plated at 8,000 cells per well; NALM-1 cells are plated at 20,000 cells per well in Costar 3903 96 well plates. After 24 hours, plates are dosed with Lerociclib at a nine-point dose concentration from 10 μM to 1 nM. Cell viability is determined after four or six days. Plates are processed on BioTek Synergy2 multi-mode plate reader and data analyzed using GraphPad Prism 5 statistical 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.
Animal Administration ^[1]	Mice^[1] Female MMTV-NEU mice are used to test the efficacy of Lerociclib (100 mpk, medicated diet). At time of treatment, body composition is assessed and weight measurements (in grams) are recorded and used as a measure of gross toxicity. Female nude mice are implanted with NSCLC PDX CTG0159 tumor. Mice are then randomized into treatment groups and dosing initiated once tumors reached a volume that fell within the range of 150-300 mm³. 100 mg/kg Lerociclib or vehicle is orally administered for 28 consecutive days. Female NCI Ath/nu mice are implanted with H1975 NSC lung adenocarcinoma model. Once tumors reach an average size of 100-150 mm³, mice are randomized into treatment cohorts. Mice are orally administered daily Afatinib (20 mg/kg), Erlotinib (70 mg/kg), or Lerociclib (50 or 100 mg/kg), as single agents or in combination (Lerociclib+Erlotinib or Lerociclib+Afatinib) for the duration of the study. All tumors are measured twice weekly until mice reach tumor burden of 1500 mm³. 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]. Bisi JE, et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343-42358.

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Lapatinib-d7 dihydrochloride(Synonyms: GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride)

发表于2024年3月17日由上海金畔生物科技有限公司

Lapatinib-d7 dihydrochloride (Synonyms: GW572016-d7 dihydrochloride; GW2016-d7 dihydrochloride)

Lapatinib-d7 (GW572016-d7) dihydrochloride 是 Lapatinib dihydrochloride 的氘代物。Lapatinib (GW572016) dihydrochloride 是一种 ErbB-2 和 EGFR 酪氨酸激酶结构域的有效抑制剂，对纯化的 EGFR 和 ErbB-2 的 IC₅₀ 值分别为 10.2 和 9.8 nM。

Lapatinib-d7 dihydrochloride Chemical Structure

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生物活性	Lapatinib-d7 (GW572016-d7) dihydrochloride is the deuterium labeled Lapatinib dihydrochloride. Lapatinib (GW572016) dihydrochloride is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC₅₀ values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively^[1].
体外研究 (In Vitro)	Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	661.02
Formula	C₂₉H₂₁D₇Cl₃FN₄O₄S
中文名称	拉帕替尼 d7 (双盐酸盐)
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.
参考文献	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [2]. Rusnak DW, et al. The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther. 2001 Dec;1(2):85-94

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TAK-960 dihydrochloride

发表于2024年3月14日由上海金畔生物科技有限公司

TAK-960 dihydrochloride 纯度: 99.81%

TAK-960 dihydrochloride 是一种有效的，可口服的，选择性的 polo-like kinase 1 (PLK1) 抑制剂，IC₅₀ 为 0.8 nM。TAK-960 dihydrochloride 对 PLK2 和 PLK3 也有抑制作用，IC₅₀ 分别为 16.9 和 50.2 nM。TAK-960 dihydrochloride 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。

TAK-960 dihydrochloride Chemical Structure

规格	价格	是否有货
10 mM * 1 mL in Water	￥2180	In-stock
5 mg	￥1300	In-stock
10 mg	￥1800	In-stock
50 mg	￥5400	In-stock
100 mg	￥8400	In-stock
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Orally Active Compound Library

生物活性

TAK-960 dihydrochloride is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC₅₀ of 0.8 nM. TAK-960 dihydrochloride also shows inhibitory activities against PLK2 and PLK3, with IC₅₀s of 16.9 and 50.2 nM, respectively. TAK-960 dihydrochloride inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts^[1].

IC₅₀ & Target^[1]

PLK1

0.8 nM (IC₅₀)

PLK2

16.9 nM (IC₅₀)

PLK3

50.2 nM (IC₅₀)

FAK/PTK2

19.6 nM (IC₅₀)

MLCK/MYLK

25.6 nM (IC₅₀)

FES/FPS

58.2 nM (IC₅₀)

体外研究
(In Vitro)

TAK-960 dihydrochloride treatment causes accumulation of G2-M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3). TAK-960 dihydrochloride (2-1000 nM; 72 hours) inhibits proliferation of multiple cancer cell lines, with mean EC₅₀ values ranging from 8.4 to 46.9 nM, but not in nondividing normal cells^[1].
TAK-960 dihydrochloride (8 nM) leads to G2/M cell cycle arrest without significant cytotoxicity in HeLa cells^[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:	HT-29, HCT116, COLO320DM, HCT-15, RKO, SW480, K-562….Hela, DU 145 cells
Concentration:	2-1000 nM
Incubation Time:	72 hours
Result:	Inhibited proliferation of human cancer cell lines regardless of TP53 and KRAS mutation and MDR1 expression status.

体内研究
(In Vivo)

TAK-960 dihydrochloride exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts^[1].
In animal models, TAK-960 dihydrochloride (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts^[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:	nude mice or SCID mice (bearing HCT116, PC-3, BT474, A549, NCI-H1299, NCI-H1975, A2780, and MV4-11 cells)^[1]
Dosage:	10 mg/kg
Administration:	P.o.; once daily for 2 weeks
Result:	Substantial antitumor activity and good tolerability.

Clinical Trial

分子量

634.52

Formula

C₂₇H₃₆Cl₂F₃N₇O₃

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 : 10 mg/mL (15.76 mM; Need ultrasonic)

DMSO : 3.23 mg/mL (5.09 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5760 mL	7.8800 mL	15.7599 mL
5 mM	0.3152 mL	1.5760 mL	3.1520 mL
10 mM	0.1576 mL	0.7880 mL	1.5760 mL

参考文献

[1]. Hikichi Y, et al. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9.

[2]. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.

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LCL521 dihydrochloride

发表于2024年3月14日由上海金畔生物科技有限公司

LCL521 dihydrochloride 纯度: 98.23%

LCL521 dihydrochloride 是一种酸性神经酰胺酶 (ACDase) 抑制剂。LCL521 还抑制溶酶体酸性鞘磷脂酶 (ASMase)。

LCL521 dihydrochloride Chemical Structure

CAS No. : 1226759-47-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥5130	In-stock
5 mg	￥3500	In-stock
10 mg	￥5500	In-stock
50 mg	￥16500	In-stock
100 mg	￥26500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

LCL521 dihydrochloride 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Metabolism/Protease Compound Library
Anti-Cancer Compound Library
Lipid Metabolism Compound Library

生物活性

LCL521 dihydrochloride is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase)^[1].

IC₅₀ & Target

ACDase, ASMase^[1]

体外研究
(In Vitro)

LCL521 (1 µM) acts as a potent inhibitor of cellular ACDase activity, whereas 10 µM LCL521 has an additional, decreased affect on the α-form of this enzyme. LCL521 (10µM) causes a time-dependent (1 hours and 5 hours) decrease of the α-ACDase form in MCF7 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

665.69

Formula

C₃₁H₅₄Cl₂N₄O₇

CAS 号

1226759-47-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 100 mg/mL (150.22 mM; Need ultrasonic)

DMSO : 20.83 mg/mL (31.29 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5022 mL	7.5110 mL	15.0220 mL
5 mM	0.3004 mL	1.5022 mL	3.0044 mL
10 mM	0.1502 mL	0.7511 mL	1.5022 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 (3.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.12 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 (3.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.12 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 (3.12 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.12 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]. Bai A, et al. Targeting (cellular) lysosomal acid ceramidase by B13: design, synthesis and evaluation of novel DMG-B13 ester prodrugs. Bioorg Med Chem. 2014 Dec 15;22(24):6933-44.

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