Vatalanib free base(Synonyms: PTK787 free base; PTK/ZK free base; CGP-79787 free base; ZK-222584 free base)

发表于2024年4月13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 free base (Synonyms: PTK787 free base; PTK/ZK free base; CGP-79787 free base; ZK-222584 free base)

Vatalanib（PTK787; ZK-222584; CGP-79787）是VEGFR2/KDR的抑制剂，其IC₅₀值为37nM。

Vatalanib free base Chemical Structure

CAS No. : 212141-54-3

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Vatalanib free base 的其他形式现货产品:

Vatalanib dihydrochloride

生物活性

Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC₅₀ of 37 nM.

IC₅₀ & Target

VEGFR2

37 nM (IC₅₀)

体外研究
(In Vitro)

Vatalanib also inhibits Flk, c-Kit and PDGFRβ with IC₅₀ of 270 nM, 730 nM and 580 nM, respectively. Vatalanib shows the anti-proliferation effect by inhibiting thymidine incorporation induced by VEGF in HUVECs with and IC₅₀ of 7.1 nM, and dose-dependently suppresses VEGF-induced survival and migration of endothelial cells in the same dose range without cytotoxic or antiproliferative effect on cells that do not express VEGF receptors^[1]. A recent study shows that Vatalanib significantly inhibits the growth of hepatocellular carcinoma cells and enhances the IFN/5-FU induced apoptosis by increasing proteins levels of Bax and reduced Bcl-xL and Bcl-2^[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)

Vatalanib induces dose-dependent inhibition of the angiogenic response to VEGF and PDGF in both a growth factor implant model and a tumor cell-driven angiogenesis model after once-daily oral dosing (25-100 mg/kg). In the same dose range, Vatalanib also inhibits the growth and metastasesof several human carcinomas in nude mice without significant effect on circulating blood cells or bone marrow leukocytes^[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

346.81

Formula

C₂₀H₁₅ClN₄

CAS 号

212141-54-3

中文名称

瓦他拉尼碱

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.

溶解性数据

In Vitro:

DMSO : 125 mg/mL (360.43 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	2.8834 mL	14.4171 mL	28.8342 mL
5 mM	0.5767 mL	2.8834 mL	5.7668 mL
10 mM	0.2883 mL	1.4417 mL	2.8834 mL

参考文献

[1]. 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

[2]. 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.

[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.

Kinase Assay ^[1]	Each GST-fused kinase is incubated under optimized buffer conditions. ATP in a total volume of 30 μL in the presence or absence of a test substance (Vatalanib) for 10 min at ambient temperature. The reaction is stopped by adding 10 μL of 250 mM EDTA^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	Subconfluent HUVECs are seeded into 96-well plates coated with 1.5% gelatin. After 24 h, growth medium is replaced by basal medium containing 1.5% FCS and a constant concentration of VEGF (50 ng/mL), bFGF (0.5 ng/mL), or FCS (5%), in the presence or absence of Vatalanib. As a control, wells without growth factor are also included. After 24 h of incubation, BrdUrd labeling solution is added, and cells incubated an additional 24 h before fixation, blocking, and addition of peroxidase-labeled anti-BrdUrd antibody. Bound antibody is then detected using 3,3′ 5,5′-tetramethylbenzidine substrate^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	A porous Teflon chamber (volume, 0.5 mL) is filled with 0.8% w/v agar containing heparin (20 units/mL) with or without growth factor (3 μg/mL human VEGF, 2 μg/mL human PDGF) is implanted s.c. on the dorsal flank of C57/C6 mice. The mice are treated with Vatalanib (12.5, 25 or 50 mg/kg dihydrochloride p.o. once daily) or vehicle (water) starting 1 day before implantation of the chamber and continuing for 5 days after. At the end of treatment, the mice are killed, and the chambers are removed. The vascularized tissue growing around the chamber is carefully removed and weighed, and the blood content is assessed by measuring the hemoglobin content of the tissue^[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]. 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 [2]. 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. [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.

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ML-9 Free Base

发表于2024年3月11日由上海金畔生物科技有限公司

ML-9 Free Base

ML-9 (Free Base) 是 Akt 激酶的选择性强效抑制剂，可抑制肌球蛋白轻链激酶 (MLCK) 和基质相互作用分子 1 (STIM1) 的活性。 ML-9 (Free Base) 抑制 MLCK，PKA 和 PKC 活性，K_i 值分别为 4、32 和 54 μM。 ML-9 通过刺激自噬小体的形成并抑制其降解来诱导自噬 (autophagy)。

ML-9 Free Base Chemical Structure

CAS No. : 110448-31-2

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

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ML-9 Free Base 的其他形式现货产品:

ML-9

生物活性

ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity^[3]. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with K_i values of 4, 32 and 54 μM, respectively^[1]. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation^[3].

体外研究
(In Vitro)

ML9 (Free Base) (0-100 μM; 0-24 hours) has no reduction in cardiomyocyte viability, 50-100 μM significantly induces cell death^[2].
ML9 (Free Base) (50 μM; 1-4 hours) significantly increases cleaved caspase-3 levels, decreased STIM1 protein levels by about 42%^[2].

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

Cell Viability Assay^[1]

Cell Line:	Neonatal rat ventricular myocytes (NRVM) cells
Concentration:	0, 10, 50 and 100 μM
Incubation Time:	0, 1, 4, 8 and 24 hours
Result:	Decreased cell viability at 50–100 μM concentration.

Apoptosis Analysis^[1]

Cell Line:	Neonatal rat ventricular myocytes (NRVM) cells
Concentration:	50 μM
Incubation Time:	0, 1, 4, 8 hours
Result:	Induced cardiomyocyte death through necrosis and apoptosis.

分子量

324.83

Formula

C₁₅H₁₇ClN₂O₂S

CAS 号

110448-31-2

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]. Ito S, et al. ML-9, a myosin light chain kinase inhibitor, reduces intracellular Ca2+ concentration in guinea pig trachealis.Eur J Pharmacol. 2004 Feb 23;486(3):325-33.

[2]. Shaikh S, et al. The STIM1 inhibitor ML9 disrupts basal autophagy in cardiomyocytes by decreasing lysosome content.Toxicol In Vitro. 2018 Apr;48:121-127.

[3]. Kondratskyi A1, et al.Identification of ML-9 as a lysosomotropic agent targeting autophagy and cell death.Cell Death Dis. 2014 Apr 24;5:e1193.

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AZD3839 free base

发表于2024年3月10日由上海金畔生物科技有限公司

AZD3839 free base 纯度: 99.98%

AZD3839 free base 是一种选择性的、具有口服活性的、可透过大脑屏障的 BACE1 抑制剂 (K_i=26 nM)。AZD3839 free base 对 BACE2 和组织蛋白酶 D 的选择性分别为 14 倍和 >1000 倍。AZD3839 free base 在小鼠、豚鼠和非人灵长类动物中表现出血浆、脑和脑脊液 Aβ 水平的剂量和时间依赖性降低。AZD3839 free base 可用于阿尔茨海默病的研究。

AZD3839 free base Chemical Structure

CAS No. : 1227163-84-9

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1430	In-stock
5 mg	￥1300	In-stock
10 mg	￥2000	In-stock
25 mg	￥4000	In-stock
50 mg	￥7000	In-stock
100 mg		询价
200 mg		询价

* Please select Quantity before adding items.

AZD3839 free base 相关产品

•相关化合物库:

Covalent Screening Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Neuronal Signaling Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
CNS-Penetrant Compound Library
Covalent Screening Library
Orally Active Compound Library
Anti-Alzheimer’s Disease Compound Library
Neurodegenerative Disease-related Compound Library

生物活性

AZD3839 free base is a potent and selective orally active, brain-permeable BACE1 inhibitor (K_i=26 nM). AZD3839 free base shows 14 and >1000-fold selectivity against BACE2 and cathepsin D, respectively. AZD3839 free base exhibits dose- and time-dependent lowering of plasma, brain, and cerebrospinal fluid Aβ levels in mouse, guinea pig, and non-human primate. AZD3839 free base can be used for the research of Alzheimer’s disease^[1]^[2].

Clinical Trial

分子量

431.41

Formula

C₂₄H₁₆F₃N₅

CAS 号

1227163-84-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 125 mg/mL (289.75 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3180 mL	11.5899 mL	23.1798 mL
5 mM	0.4636 mL	2.3180 mL	4.6360 mL
10 mM	0.2318 mL	1.1590 mL	2.3180 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。-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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 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 (4.82 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.82 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]. Sparve E et al. Prediction and modeling of effects on the QTc interval for clinical safety margin assessment, based on single-ascending-dose study data with AZD3839. J Pharmacol Exp Ther. 2014 Aug;350(2):469-78.

[2]. Jeppsson F et al. Discovery of AZD3839, a potent and selective BACE1 inhibitor clinical candidate for the treatment of Alzheimer disease. J Biol Chem. 2012 Nov 30;287(49):41245-57.

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AV-412 free base(Synonyms: MP-412 free base)

发表于2024年3月6日由上海金畔生物科技有限公司

AV-412 free base (Synonyms: MP-412 free base) 纯度: 98.07%

AV-412 free base (MP-412 free base) 是 EGFR 抑制剂，抑制EGFR，EGFR^L858R，EGFR^T790M，EGFR^L858R/T790M 和 ErbB2的 IC₅₀ 值分别为0.75，0.5，0.79，2.3，19 nM。

AV-412 free base Chemical Structure

CAS No. : 451492-95-8

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2008	In-stock
2 mg	￥1100	In-stock
5 mg	￥1800	In-stock
10 mg	￥2800	In-stock
50 mg	￥8800	In-stock
100 mg	￥13500	In-stock
200 mg		询价
500 mg		询价

* Please select Quantity before adding items.

AV-412 free base 相关产品

•相关化合物库:

Covalent Screening Library Plus
Clinical Compound Library Plus
Bioactive Compound Library Plus
Immunology/Inflammation Compound Library
JAK/STAT Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Clinical Compound Library
Covalent Screening Library
Differentiation Inducing Compound Library
Anti-Hepatitis C Virus Compound Library
Anti-Breast Cancer Compound Library
Anti-Lung Cancer Compound Library
Anti-Pancreatic Cancer Compound Library
Angiogenesis Related Compound Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC₅₀s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M and ErbB2, respectively.

IC₅₀ & Target^[1]

EGFR

0.75 nM (IC₅₀)

ErbB2

19 nM (IC₅₀)

EGFR^L858R

0.51 nM (IC₅₀)

EGFR^L858R/T790M

2.3 nM (IC₅₀)

EGFR^T790M

0.79 nM (IC₅₀)

体外研究
(In Vitro)

AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC₅₀ of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC₅₀ of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR^[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 animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib^[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

507.00

Formula

C₂₇H₂₈ClFN₆O

CAS 号

451492-95-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 50 mg/mL (98.62 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9724 mL	9.8619 mL	19.7239 mL
5 mM	0.3945 mL	1.9724 mL	3.9448 mL
10 mM	0.1972 mL	0.9862 mL	1.9724 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 (4.93 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.93 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

*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]. Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptorand ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.

Kinase Assay ^[1]	Recombinant intracellular kinase domains of EGFR, EGFR^L858R, EGFR^T790M, EGFR^L858R/T790M, and purified EGFR from A431 cell membranes are used. Kinase reactions are carried out in 8 mM MOPS (pH 7.0), 0.2 mM ethylenediaminetetraacetic acid (EDTA), 10 mM MnCl₂, 10 mM Mg acetate, 0.1 mg/mL poly(Glu, Tyr) 4:1, [γ³³P-ATP], and 5–10 mU of enzyme, except that 250 µM of the GGMEDIYFEFMGGKKK peptide substrate is used for EGFR^T790M. Phosphorylation is initiated by the addition of ATP and is allowed to proceed for 40 min at room temperature. The reaction is stopped by the addition of 3% phosphoric acid, then aliquots of the reaction mixture are spotted onto a filtermat. After rinsing to remove peptides bound non-specifically, the filter is scintillation counted^[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]	To test the effects of AV-412 on growth factor-dependent cell proliferation, A431 and A7r5 cells are cultured for 24 h at 37°C in the presence of 1 ng/mL epidermal growth factor and 50 ng/mL platelet-derived growth factor, respectively. The ³H-thymidine incorporation during this period is measured^[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: For studies examining the dosing schedule in relation to efficacy against TE-8 tumors, AV-412 is administered either once daily, every other day, or once per week for 2 weeks. Mice are killed 1 day after the final treatment, and the tumors are dissected and weighed. For evaluation of tumor phosphorylation, tumor-bearing mice are given a single administration of AV-412 and tumors are dissected 4 h later^[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]. Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptorand ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.

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多肽定制Goserelin (free base) 编码 [65807-02-5]

发表于2024年2月27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可以定制不同序列多肽，可以访问官网了解更多产品信息。

名称	Goserelin (free base)
编码	[65807-02-5]
别名	Goserelin (free base)
纯度	80%，90%，95%，98%，99%
重量	1mg,5mg,10mg,50mg,100mg,1g
序列（单字母缩写）	Pyr-HWSYs(tBu)-LRP-Azagly-NH2
序列（三字母缩写）	Pyr-His-Trp-Ser-Tyr-D-Ser(tBu)-Leu-Arg-Pro-Azagly-NH2?(trifluoroacetate salt)
基本描述	The GnRH II sequence pEHWSHGWYPG amide, first detected in chicken, is highly conserved in vertebrates.
溶解度
分子量	1269.43
化学式	C59H84N18O14
存储条件	Store at -20°C. Keep tightly closed. Store in a cool dry place.
注释
Documents
Figures
Reference	A.Wells et al., Clin. Cancer Res., 8, 1251 (2002) A.Rody et al., Expert Rev. Anticancer Ther., 5, 591 (2005) H.Lepor, Rev. Urol., 7 (Suppl. 5), S3 (2005) Merck Index, 14th ed., No. 4526, (2006) M.Roach 3rd and A.Izaguirre, Expert Opin. Pharmacother., 8, 257 (2007) R.M.Herrmann et al., Rad. Oncol., 2, 31 (2007)
C端
N端
化学桥

ZW4864 free base

发表于2024年2月21日由上海金畔生物科技有限公司

ZW4864 free base 纯度: 99.38%

ZW4864 (free base) 是一种具有口服活性和选择性的 β catenin/ B-Cell lymphoma 9 蛋白-蛋白相互作用 (β catenin/BCL9 PPI) 抑制剂。ZW4864 (free base) 抑制 β catenin/BCL9 PPI 的 K_i 值为 0.76 μM，IC₅₀ 值为 0.87 μM。

ZW4864 free base Chemical Structure

CAS No. : 2632259-92-6

规格	价格	是否有货
5 mg	￥5000	In-stock
10 mg	￥8500	In-stock
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ZW4864 free base 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Stem Cell Signaling Compound Library
Wnt/Hedgehog/Notch Compound Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Differentiation Inducing Compound Library
Cytoskeleton Compound Library
Orally Active Compound Library
Neuroprotective Compound Library
Anti-Breast Cancer Compound Library
Anti-Blood Cancer Compound Library
Transcription Factor Targeted Library
Anti-Liver Cancer Compound Library
Anti-Colorectal Cancer Compound Library

生物活性

ZW4864 (free base) is an orally active and selective β catenin/B-Cell lymphoma 9 protein−protein interaction (β catenin/BCL9 PPI) inhibitor. ZW4864 (free base) inhibits β catenin/BCL9 PPI with a K_i value of 0.76 μM and an IC₅₀ value of 0.87 μM^[1].

IC₅₀ & Target

IC50: 0.87 μM (β catenin/BCL9 PPI)^[1].
Ki: 0.76 μM (β catenin/BCL9 PPI)^[1]

体外研究
(In Vitro)

ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) decreases the expression levels of Axin2 and cyclin D1 proteins^[1].
ZW4864 (10~40 μM; 72 hours; MDA-MB231, MCF10A and MDA-MB-468 cells) (free base) selectively triggeres rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells^[1].
ZW4864 (10~40 μM; 24 hours; SW480 and MBA-MD-231 cells) (free base) suppresses the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells^[1].
ZW4864 (free base) binds with β-catenin and selectively disrupts the protein−protein interaction (PPI) between B-cell lymphoma 9 (BCL9) and β-catenin while sparing the β-catenin/E-cadherin PPI. ZW4864 (free base) dose-dependently suppresses β-catenin signaling activation, downregulates oncogenic β-catenin target genes, and abrogates invasiveness of β-catenin-dependent cancer cells. ZW4864 (free base) suppresses TOPFlash luciferase activities in β-catenin expressing HEK293 cells in a dose-dependent manner with an IC₅₀ of 11 μM. ZW4864 (free base) also dose-dependently suppresses the TOPFlash luciferase activities in SW480 and Wnt 3a-activated MDA-MB-468 cells with the IC₅₀s of 7.0 and 6.3 μM, respectively. ZW4864 (free base) selectively suppresses transactivation of β-catenin signaling^[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:	SW480 and MBA-MD-231 cells
Concentration:	10~40 μM
Incubation Time:	24 hours
Result:	Decreased the expression levels of Axin2 and cyclin D1 proteins.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB231, MCF10A and MDA-MB-468 cells
Concentration:	10~40 μM
Incubation Time:	72 hours
Result:	Selectively triggered rapid apoptosis of triple-negative breast cancer cells with hyperactive β-catenin signaling while sparing normal mammary epithelial MCF10A cells.

RT-PCR^[1]

Cell Line:	SW480 and MBA-MD-231 cells
Concentration:	10~40 μM
Incubation Time:	24 hours
Result:	Suppressed the transcription of β-catenin target genes in a concentration-dependent manner without affecting the expression of HPRT, a house-keeper gene, in both SW480 and Wnt 3a-activated MDA-MB-231 cells.

体内研究
(In Vivo)

ZW4864 (20 mg/kg; p.o.) (free base) exhibits good pharmacokinetic properties with an oral bioavailability (F) of 83 %^[1].
ZW4864 (90 mg/kg; p.o.) (free base) shows a variation in tumor growth in mice^[1].
ZW4864 (free base) shows good pharmacokinetic properties and effectively suppresses β-catenin target gene expression in the patient-derived xenograft mouse 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.

Animal Model:	C57BL/6 mice^[1]
Dosage:	20 mg/kg (Pharmacokinetic Analysis)
Administration:	P.o.
Result:	Exhibited good pharmacokinetic properties with an oral bioavailability (F) of 83%.

Animal Model:	Mice^[1]
Dosage:	90 mg/kg
Administration:	P.o.
Result:	Showed a variation in tumor growth in mice.

分子量

570.72

Formula

C₃₃H₄₂N₆O₃

CAS 号

2632259-92-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Wang Z, et al. Discovery of an Orally Bioavailable Small-Molecule Inhibitor for the β-Catenin/B-Cell Lymphoma 9 Protein-Protein Interaction. J Med Chem. 2021;64(16):12109-12131.

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AS-99 free base

发表于2024年2月20日由上海金畔生物科技有限公司

AS-99 free base

AS-99 是首创的、有效的、选择性的 ASH1L 组蛋白甲基转移酶抑制剂 (IC₅₀= 0.79 µM, K_d= 0.89 µM)，具有抗白血病活性。AS-99 在体内阻断细胞增殖，诱导细胞凋亡 (apoptosis) 和分化，下调 MLL 融合靶基因，减轻白血病。

AS-99 free base Chemical Structure

CAS No. : 2323623-93-2

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10 mg	￥9800	询问价格 & 货期
25 mg	￥19000	询问价格 & 货期
50 mg	￥32000	询问价格 & 货期
100 mg	￥50000	询问价格 & 货期

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AS-99 free base 的其他形式现货产品:

AS-99 TFA

生物活性

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC₅₀= 0.79 µM, K_d= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo^[1].

IC₅₀ & Target

0.79 µM (ASH1L histone methyltransferase)^[1]

体外研究
(In Vitro)

AS-99 is tested against a panel of 20 histone methyltransferases, including NSD1, NSD2, NSD3, and SETD2. NO significant inhibition is observed at 50 µM of AS-99 on any of the tested histone methyltransferases, indicating over 100-fold selectivity towards ASH1L^[1].
AS-99 shows a several fold weaker effect on the proliferation of leukemia cells without MLL1 translocations, such as SET2 and K562, with no or limited effects at 10 µM or higher concentrations^[1].
AS-99 (1-8 µM; 7 days) also induces apoptosis in the MLL leukemia cells, but not in the K562 cells, as assessed by the quantification of the Annexin V positive cells^[1].
AS-99 suppresses MLL fusion driven transcriptional programs^[1].
AS-99 results in a reduced number of H3K36me2 peaks when compared to the DMSO-treated 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.

RT-PCR^[1]

Cell Line:	MOLM13 cells
Concentration:	2-6 µM
Incubation Time:	7 days
Result:	Led to a dose-dependent downregulation of canonical MLL fusion target genes required for leukemogenesis including MEF2C, DLX2, FLT3, and HOXA9.

体内研究
(In Vivo)

AS-99 (30 mg/kg; i.p.; q.d., treated for 14 consecutive days) reduces leukemia burden in mice^[1].
AS-99 is used for in vivo studies in mice, which reveals favorable exposure in plasma upon i.v. and i.p. administration (AUC = 9701 hr* ng/mL and 10,699 hr* ng/mL, respectively), suitable half-life (~5–6 h) and Cmax >10 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.

Animal Model:	8- to 10-week old female NSG mice (bearing MV4;11 cells)^[1]
Dosage:	30 mg/kg
Administration:	I.p.; q.d., treated for 14 consecutive days
Result:	Reduced the leukemia burden in the xenotransplantation mouse model of MLL leukemia without affecting blood counts in normal mice.

分子量

593.68

Formula

C₂₇H₃₀F₃N₅O₃S₂

CAS 号

2323623-93-2

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]. David S. Rogawski, Jing Deng, Hao Li, Tomasz Cierpicki, Jolanta Grembecka, et al. Discovery of first-in-class inhibitors of ASH1L histone methyltransferase with anti-leukemic activity. Nat Commun. 2021 May 14;12(1):2792.

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Phortress free base

发表于2024年1月20日由上海金畔生物科技有限公司

Phortress free base

Phortress free base (NSC 710305)是一种 P450 CYP1A1 激活的抗肿瘤前药，具有抗肿瘤活性。 Phortress free base导致DNA损伤和细胞周期停滞。

Phortress free base Chemical Structure

CAS No. : 741241-36-1

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生物活性	Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity^[1]. Phortress free base leads to DNA damage and cell cycle arrest^[2].
分子量	386.49
Formula	C₂₀H₂₃FN₄OS
CAS 号	741241-36-1
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]. Behrsing HP, et al. In vitro exposure of precision-cut lung slices to 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride (NSC 710305, Phortress) increases inflammatory cytokine content and tissue damage. Toxicol Sci. 2013 Feb;131(2):470-9. [2]. Trapani V, et al. DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells. Br J Cancer. 2003 Feb 24;88(4):599-605.

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Phortress free base

发表于2024年1月20日由上海金畔生物科技有限公司

Phortress free base

Phortress free base (NSC 710305)是一种 P450 CYP1A1 激活的抗肿瘤前药，具有抗肿瘤活性。 Phortress free base导致DNA损伤和细胞周期停滞。

Phortress free base Chemical Structure

CAS No. : 741241-36-1

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

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生物活性	Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity^[1]. Phortress free base leads to DNA damage and cell cycle arrest^[2].
分子量	386.49
Formula	C₂₀H₂₃FN₄OS
CAS 号	741241-36-1
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]. Behrsing HP, et al. In vitro exposure of precision-cut lung slices to 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride (NSC 710305, Phortress) increases inflammatory cytokine content and tissue damage. Toxicol Sci. 2013 Feb;131(2):470-9. [2]. Trapani V, et al. DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells. Br J Cancer. 2003 Feb 24;88(4):599-605.

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

Phortress free base

发表于2024年1月20日由上海金畔生物科技有限公司

Phortress free base

Phortress free base (NSC 710305)是一种 P450 CYP1A1 激活的抗肿瘤前药，具有抗肿瘤活性。 Phortress free base导致DNA损伤和细胞周期停滞。

Phortress free base Chemical Structure

CAS No. : 741241-36-1

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	Phortress free base (NSC 710305) is a P450 CYP1A1-activated antitumor prodrug with antitumor activity^[1]. Phortress free base leads to DNA damage and cell cycle arrest^[2].
分子量	386.49
Formula	C₂₀H₂₃FN₄OS
CAS 号	741241-36-1
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]. Behrsing HP, et al. In vitro exposure of precision-cut lung slices to 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole lysylamide dihydrochloride (NSC 710305, Phortress) increases inflammatory cytokine content and tissue damage. Toxicol Sci. 2013 Feb;131(2):470-9. [2]. Trapani V, et al. DNA damage and cell cycle arrest induced by 2-(4-amino-3-methylphenyl)-5-fluorobenzothiazole (5F 203, NSC 703786) is attenuated in aryl hydrocarbon receptor deficient MCF-7 cells. Br J Cancer. 2003 Feb 24;88(4):599-605.

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

GW768505A free base

发表于2024年1月20日由上海金畔生物科技有限公司

GW768505A free base

GW768505A free base 是高效的 VEGFR2 (KDR) 和Tie-2 双抑制剂，对 VEGFR2 作用的 pIC₅₀ 值为 7.81。GW768505A free base 具有抗血管生成活性。

GW768505A free base Chemical Structure

CAS No. : 501693-25-0

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生物活性

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity^[1]。

IC₅₀ & Target

KDR

Tie-2

体外研究
(In Vitro)

GW768505A free base has inhibition for cancer cells growth in NCI-60 panel screening^[2].
GW768505A free base is an inhibitor of KDR and TIE2, shows potent inhibition (71–88% inhibition at 100 nM) of the tropomysin-related kinases TRKA, TRKB and TRKC^[2].

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

分子量

537.47

Formula

C₂₇H₁₉F₄N₅O₃

CAS 号

501693-25-0

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]. Miyazaki Y, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

[2]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103.

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GW768505A free base

发表于2024年1月20日由上海金畔生物科技有限公司

GW768505A free base

GW768505A free base 是高效的 VEGFR2 (KDR) 和Tie-2 双抑制剂，对 VEGFR2 作用的 pIC₅₀ 值为 7.81。GW768505A free base 具有抗血管生成活性。

GW768505A free base Chemical Structure

CAS No. : 501693-25-0

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

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生物活性

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity^[1]。

IC₅₀ & Target

KDR

Tie-2

体外研究
(In Vitro)

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

537.47

Formula

C₂₇H₁₉F₄N₅O₃

CAS 号

501693-25-0

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]. Miyazaki Y, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

[2]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103.

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

GW768505A free base

发表于2024年1月20日由上海金畔生物科技有限公司

GW768505A free base

GW768505A free base 是高效的 VEGFR2 (KDR) 和Tie-2 双抑制剂，对 VEGFR2 作用的 pIC₅₀ 值为 7.81。GW768505A free base 具有抗血管生成活性。

GW768505A free base Chemical Structure

CAS No. : 501693-25-0

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

GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC₅₀ of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity^[1]。

IC₅₀ & Target

KDR

Tie-2

体外研究
(In Vitro)

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

分子量

537.47

Formula

C₂₇H₁₉F₄N₅O₃

CAS 号

501693-25-0

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]. Miyazaki Y, et al. Orally active 4-amino-5-diarylurea-furo[2,3-d]pyrimidine derivatives as anti-angiogenic agent inhibiting VEGFR2 and Tie-2. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1773-8.

[2]. Elkins JM, et al. Comprehensive characterization of the Published Kinase Inhibitor Set. Nat Biotechnol. 2016 Jan;34(1):95-103.

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

BPH-1358 free base(Synonyms: NSC50460 free base)

发表于2024年1月19日由上海金畔生物科技有限公司

BPH-1358 free base (Synonyms: NSC50460 free base)

BPH-1358 free base (NSC50460 free base) 是一种有效的人 FPPS 和 UPPS 抑制剂，IC₅₀ 值分别为 1.8 μM 和 110 nM，在体外对金黄色葡萄球菌的 MIC 值大约为 250 ng/mL。

BPH-1358 free base Chemical Structure

CAS No. : 801985-13-7

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

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生物活性	BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against *S. aureus* in vitro (MIC ~250 ng/mL)^[1]^[2].
IC₅₀ & Target	IC50: 1.8 μM (human bisphosphonate farnesyl diphosphate synthase)^[1]; 100 nM (undecaprenyl diphosphate synthase)^[2]
体外研究 (In Vitro)	BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC₅₀ of 110 nM. BPH-1358 against E. coli and S. aureus with EC₅₀ of 300 nM and 290 nM, respectively^[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)	BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	528.60
Formula	C₃₂H₂₈N₆O₂
CAS 号	801985-13-7
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]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27. [2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349-54.

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BPH-1358 free base(Synonyms: NSC50460 free base)

发表于2024年1月19日由上海金畔生物科技有限公司

BPH-1358 free base (Synonyms: NSC50460 free base)

BPH-1358 free base Chemical Structure

CAS No. : 801985-13-7

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	BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against *S. aureus* in vitro (MIC ~250 ng/mL)^[1]^[2].
IC₅₀ & Target	IC50: 1.8 μM (human bisphosphonate farnesyl diphosphate synthase)^[1]; 100 nM (undecaprenyl diphosphate synthase)^[2]
体外研究 (In Vitro)	BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC₅₀ of 110 nM. BPH-1358 against E. coli and S. aureus with EC₅₀ of 300 nM and 290 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.
体内研究 (In Vivo)	BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)^[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	528.60
Formula	C₃₂H₂₈N₆O₂
CAS 号	801985-13-7
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]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27. [2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349-54.

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BPH-1358 free base(Synonyms: NSC50460 free base)

发表于2024年1月19日由上海金畔生物科技有限公司

BPH-1358 free base (Synonyms: NSC50460 free base)

BPH-1358 free base Chemical Structure

CAS No. : 801985-13-7

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	BPH-1358 free base (NSC50460 free base) is a potent human farnesyl diphosphate synthase (FPPS) and undecaprenyl diphosphate synthase (UPPS) inhibitor with IC₅₀s of 1.8 μM and 110 nM, respectively, and is active against *S. aureus* in vitro (MIC ~250 ng/mL)^[1]^[2].
IC₅₀ & Target	IC50: 1.8 μM (human bisphosphonate farnesyl diphosphate synthase)^[1]; 100 nM (undecaprenyl diphosphate synthase)^[2]
体外研究 (In Vitro)	BPH-1358 is the most potent inhibitor of both E. coli UPPS (EcUPPS) as well as S. aureus UPPS (SaUPPS) with an IC₅₀ of 110 nM. BPH-1358 against E. coli and S. aureus with EC₅₀ of 300 nM and 290 nM, respectively^[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)	BPH-1358 is active against S. aureus in vivo (20/20 mice survived in an i.p. infection model with a MRSA strain)^[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量	528.60
Formula	C₃₂H₂₈N₆O₂
CAS 号	801985-13-7
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]. Zhu W, et al. Antibacterial drug leads: DNA and enzyme multitargeting. J Med Chem. 2015 Feb 12;58(3):1215-27. [2]. Liu YL, et al. Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries. ACS Med Chem Lett. 2015 Jan 29;6(3):349-54.

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BRD7-IN-1 free base

发表于2023年11月7日由上海金畔生物科技有限公司

BRD7-IN-1 free base

BRD7-IN-1 free base 是一种修饰的 BI7273 衍生物 (BRD7/9 抑制剂)，通过与 VHL 配体连接形成 PROTAC VZ185 (VZ185 抑制 BRD7/9 的 DC₅₀ 分别是 4.5 nM、1.8 nM)。

BRD7-IN-1 free base Chemical Structure

CAS No. : 2305379-66-0

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生物活性	BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC₅₀s of 4.5 and 1.8 nM, respectively)^[1].
IC₅₀ & Target	BRD7, BRD9^[1]
分子量	394.47
Formula	C₂₂H₂₆N₄O₃
CAS 号	2305379-66-0
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]. Zoppi V, et al. Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7. J Med Chem. 2019 Jan 24;62(2):699-726.

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R406 free base

发表于2023年11月4日由上海金畔生物科技有限公司

R406 free base 纯度: 99.69%

R406 free base 是一种有效的，具有口服活性的，ATP竞争性的 Syk/FLT3 抑制剂，K_i 为 30 nM，有效抑制 Syk 激酶活性，IC₅₀ 为 41 nM。R406 free base 可减轻免疫复合物介导的炎症。R406 free base 还抑制 Lyn (IC₅₀=63 nM) 和 Lck (IC₅₀=37 nM).

R406 free base Chemical Structure

CAS No. : 841290-80-0

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥1729	In-stock
2 mg	￥810	In-stock
5 mg	￥1250	In-stock
10 mg	￥1989	In-stock
50 mg	￥6412	In-stock
100 mg	￥10114	In-stock
200 mg		询价
500 mg		询价

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R406 free base 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Apoptosis Compound Library
Immunology/Inflammation Compound Library
Kinase Inhibitor Library
Protein Tyrosine Kinase Compound Library
Anti-Cancer Compound Library
Diabetes Related Compound Library
Anti-Lung Cancer Compound Library
Anti-Blood Cancer Compound Library

生物活性

R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk kinase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 free base reduces immune complex-mediated inflammation^[1]. R406 free base also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM)^[2].

IC₅₀ & Target

Ki: 30 nM (Syk)^[1]
IC50: 41 nM (Syk)^[1]
FLT3^[1]
IC50: 63 nM (Lyn), 37 nM (Lck)^[2]

体外研究
(In Vitro)

R406 inhibits adenosine A3 receptor (IC₅₀=0.081 µM), adenosine transporter (IC₅₀=1.84 µM), and monoamine transporter (IC₅₀=2.74 µM)^[1].
R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC₅₀s of 15.1, 2.9 and 6.3 µM, respectively^[1].
R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B 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:	Cultured human mast cells (CHMC)
Concentration:	0.016, 0.08, 0.4, 2 µM
Incubation Time:	40 minutes
Result:	Inhibited all other kinases tested at 5 to 100 fold less potency than Syk as judged by phosphorylation of target proteins.

体内研究
(In Vivo)

R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406^[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:	Female Balb/c mice (6-8 weeks) with CAIA^[1]
Dosage:	5 and 10 mg/kg
Administration:	Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
Result:	Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.

Animal Model:	Female C57BL/6 mice with arthritis^[1]
Dosage:	10 mg/kg
Administration:	Administered orally one hour before serum injection; b.i.d; for 13 days
Result:	Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.

分子量

470.45

Formula

C₂₂H₂₃FN₆O₅

CAS 号

841290-80-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : ≥ 10 mg/mL (21.26 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	2.1256 mL	10.6281 mL	21.2562 mL
5 mM	0.4251 mL	2.1256 mL	4.2512 mL
10 mM	0.2126 mL	1.0628 mL	2.1256 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: ≥ 0.5 mg/mL (1.06 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.06 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 5.0 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% corn oil

Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.06 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 5.0 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]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.

[2]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8.

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AFP464 free base(Synonyms: NSC710464 free base)

发表于2023年10月31日由上海金畔生物科技有限公司

AFP464 free base (Synonyms: NSC710464 free base)

AFP464 free base (NSC710464 free base) 是一种有效的 HIF-1α 抑制剂，IC₅₀ 值为 0.25 μM。同时也是 aryl hydrocarbon receptor (AhR) 的激活剂。

AFP464 free base Chemical Structure

CAS No. : 468719-52-0

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生物活性

AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC₅₀ of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.

IC₅₀ & Target

IC50：0.25 μM (HIF-1α)^[1]

Clinical Trial

分子量

448.44

Formula

C₂₂H₂₃F₃N₄O₃

CAS 号

468719-52-0

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]. Terzuoli E1, Aminoflavone, a ligand of the aryl hydrocarbon receptor, inhibits HIF-1alpha expression in an AhR-independent fashion. Cancer Res. 2010 Sep 1;70(17):6837-48.

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Toremifene(Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

发表于2023年9月20日由上海金畔生物科技有限公司

Toremifene (Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)

Toremifene (Z-Toremifene) 是第二代选择性雌激素受体调节剂，对雌激素受体的 IC₅₀ 为 1μM。Toremifene 还可以有效抑制传染性 EBOV Zaire 和 Marburg (MARV)，IC₅₀ 分别为 0.07 µM 和 2.6 µM。

Toremifene Chemical Structure

CAS No. : 89778-26-7

规格		是否有货
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Toremifene 的其他形式现货产品:

Toremifene citrate

生物活性

Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.07 µM and 2.6 µM, respectively^[1]^[2].

体外研究
(In Vitro)

Toremifene is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis and other adverse effects resulting from ADT with prostate cancer^[1].
The growth of Ac-1 cells was inhibited by tamoxifen, toremifene and atamestane in vitro with IC50values of 1.8±1.3μM, 1±0.3μM and 60.4±17.2μM, respectively. The combination of toremifene plusatamestane was found to be better than toremifene or atamestane alone in vitro^[3].

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)

The effect of this combination was then studied in vivo using Ac-1 xenografts grown in ovariectomized female SCID mice. The mice were injected with toremifene (1000μg/day), atamestane (1000μg/day), tamoxifen (100μg/day), or the combination of toremifene plus atamestane. In this study, our results indicate that the combination of toremifene plus atamestane was as effective as toremifene or tamoxifen alone but may not provide any additional benefit over toremifene alone or tamoxifen alone^[3].

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

Clinical Trial

分子量

405.96

Formula

C₂₆H₂₈ClNO

CAS 号

89778-26-7

中文名称

托瑞米芬；涛瑞米芬

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]. Matthew R Smith, Selective Estrogen Receptor Modulators to Prevent Treatment-Related Osteoporosis.Rev Urol. 2005; 7(Suppl 3): S30-S35.

[2]. Laura Cooper, et al. Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. J Med Chem. 2020 Sep 4.

[3]. Gauri J Sabnis, Luciana Macedo, Olga Goloubeva, Toremifene – Atamestane; Alone or In Combination: Predictions from the Preclinical Intratumoral Aromatase Model. J Steroid Biochem Mol Biol. 2008 January; 108(1-2): 1-7.

[4]. Taneja SS, Morton R, Barnette G, Prostate cancer diagnosis among men with isolated high-grade intraepithelial neoplasia enrolled onto a 3-year prospective phase III clinical trial of oral toremifene. J Clin Oncol. 2013 Feb 10;31(5):523-9.

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赛默飞Alfa aesar官网

赛默飞Acros试剂中国官网 Alfa aesar阿法埃莎中国代理商

标签归档：base

Vatalanib free base(Synonyms: PTK787 free base; PTK/ZK free base; CGP-79787 free base; ZK-222584 free base)

ML-9 Free Base

AZD3839 free base

AZD3839 free base 相关产品

•相关化合物库:

AV-412 free base(Synonyms: MP-412 free base)

AV-412 free base 相关产品

•相关化合物库:

多肽定制Goserelin (free base) 编码 [65807-02-5]

ZW4864 free base

ZW4864 free base 相关产品

•相关化合物库:

AS-99 free base

Phortress free base

Phortress free base

Phortress free base

GW768505A free base

GW768505A free base

GW768505A free base

BPH-1358 free base(Synonyms: NSC50460 free base)

BPH-1358 free base(Synonyms: NSC50460 free base)

BPH-1358 free base(Synonyms: NSC50460 free base)

BRD7-IN-1 free base

R406 free base

R406 free base 相关产品

•相关化合物库:

AFP464 free base(Synonyms: NSC710464 free base)

Toremifene(Synonyms: Z-Toremifene; NK 622 free base; FC-1157a free base)