ZSQ836 | CDK12/13 inhibitor | Probechem Biochemicals

Chemical Structure : ZSQ836

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ZSQ836 (ZSQ 836)

货号: PC-49260Not For Human Use, Lab Use Only.

ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.

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生物&药学活性

ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.
ZSQ836 shows weak affinity (CDK9, GSK3A, and GSK3B) against a panel of 373 other kinases, exhibits comparable selectivity of organoarsenic CDK12/CDK13 covalent inhibitors to THZ531.
ZSQ836 is a potent antagonist against ovarian cancer, provokes DNA damage in ovarian cancer.
ZSQ836 is orally bioavailable and impairs tumor growth in vivo, and is efficacious in a murine ovarian tumor model.
ZSQ836 suppresses T cell proliferation and activation.

物理化学性质&存储条件

分子量	627.054
分子式	C27H28AsClN6OS2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(R)-N-(4-(1,3,2-dithiarsolan-2-yl)phenyl)-2-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidin-1-yl)acetamide

参考文献

1. Lin Cheng, et al. Cancer Res. 2022 Jul 20;CAN-22-0222.

ZSQ836 (ZSQ 836)

生物&药学活性

物理化学性质&存储条件

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ZSQ836 (ZSQ 836)

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物理化学性质&存储条件

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