ZLC491 | CDK12/13 PROTAC | Probechem Biochemicals

Chemical Structure : ZLC491

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ZLC491 (ZLC-491)

货号: PC-23155Not For Human Use, Lab Use Only.

ZLC491 is a potent, selective, and orally bioavailable CDK12/13 PROTAC degrader with DC50 values of 32 and 28 nM, respectively, in TNBC MDA-MB-231 cells.

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生物&药学活性

ZLC491 is a potent, selective, and orally bioavailable CDK12/13 PROTAC degrader with DC50 values of 32 and 28 nM, respectively, in TNBC MDA-MB-231 cells.
ZLC491 selectively induces CDK12/13 degradation in a cereblon- and proteasome-dependent manner.
ZLC491 is able to deplete CDK12/13 in a concentration-dependent manner in other TNBC cells including HCC38 and MDA-MB-436 cells.
ZLC491 is highly selective for CDK12 over other CDKs.
ZLC491 effectively reduces DDR gene expression and potently inhibited TNBC cell growth alone or combined with DNA damaging agents or PARP inhibitors.
ZLC491 potently inhibits the growth of MDA-MB-231, HCC38, and MDA-MB-436 cells with IC50 values of 0.62, 0.19 and 0.12 μM, respectively.
ZLC491 (100-200 mg/kg, p.o.) depleted CDK12 and CDK13 proteins, induced apoptotic cell death in the tumors in MDA-MB-231 xenografts model.

物理化学性质&存储条件

分子量	867.00
分子式	C48H51FN10O5
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	3-Benzyl-1-((1r,4r)-4-((5-cyanopyridin-2-yl)amino)cyclohexyl)-1-(4-(4-(1-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperidin-4-yl)piperazin-1-yl)phenyl)urea

参考文献

1. Licheng Zhou, et al. J Med Chem. 2024 Oct 10. doi: 10.1021/acs.jmedchem.4c01596.

ZLC491 (ZLC-491)

生物&药学活性

物理化学性质&存储条件

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ZLC491 (ZLC-491)

生物&药学活性

物理化学性质&存储条件

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