GW806742X hydrochloride-武汉科斯坦生物科技有限公司

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GW806742X hydrochloride

英文名称：GW806742X hydrochloride

品牌：Chemstan

货号：CS-112292A

价格： ￥600/mg
发布日期： 2021-03-10
更新日期： 2025-09-19

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产地
品牌	Chemstan
货号	CS-112292A
用途	科研
英文名称	GW806742X hydrochloride
包装规格	5 mg
纯度	98%%
CAS编号
别名
分子式
是否进口	否

Description

GW806742X hydrochloride, an ATP mimetic and a potent MLKL (Mixed Lineage Kinase Domain-Like protein) inhibitor, binds the MLKL pseudokinase domain with a K_d of 9.3 μM. GW806742X hydrochloride has activity against VEGFR2 (IC₅₀=2 nM). GW806742X hydrochloride retards MLKL membrane translocation and inhibits necroptosis^[1]^[2].

IC₅₀ & Target^[1]^[2]

MLKL

9.3 μM (Kd)

VEGFR2

2 nM (IC₅₀)

In Vitro

GW806742X (0.1-10000 nM) inhibits necroptotic death of wild-type mouse dermal fibroblasts (MDFs) stimulated with TSQ (1 ng/mL TNF, 500 nM compound A (Smac mimetic), 10 μM Q-VD-OPh) in a dose-dependent manner^[1].
GW806742X shows inhibition of VEGF induced proliferation of HUVECs with an IC50 of 5 nM^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

610.01

Formula

C??H??ClF?N?O?S

SMILES

[H]Cl.O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (163.93 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic) (insoluble)

Preparing
Stock Solutions

ConcentrationSolventMass	1 mg	5 mg	10 mg

1 mM	1.6393 mL	8.1966 mL	16.3932 mL
5 mM	0.3279 mL	1.6393 mL	3.2786 mL
10 mM	0.1639 mL	0.8197 mL	1.6393 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 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.10 mM); Clear solution

*以上所有助溶剂都可在 MCE 网站选购。

References

[1]. Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014;111(42):15072-15077.

[2]. Sammond DM, et al. Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase. Bioorg Med Chem Lett. 2005;15(15):3519-3523.