MFH290 | CDK12/13 inhibitor | Probechem Biochemicals

Chemical Structure : MFH290

CAS No.: 2088715-91-5

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MFH290 (MFH-290, MFH 290)

货号: PC-72216Not For Human Use, Lab Use Only.

MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.

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10 mg	￥7280	In stock
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生物&药学活性

MFH290 (MFH-290) is a potent, highly selective, covalent inhibitor of CDK12/13 with IC50 of 25/49 nM.
MFH290 forms a covalent bond with Cys-1039 of CDK12, and CDK12-dependent as mutation of Cys-1039 rendered the kinase refractory to MFH290.
MFH290 exhibits excellent kinome selectivity, inhibits the phosphorylation of serine-2 in the C-terminal domain (CTD) of RNA-polymerase II (Pol II), and reduces the expression of key DNA damage repair genes.
MFH290 restored Pol II CTD phosphorylation and DNA damage repair gene expression AND augments the antiproliferative effect of the PARP inhibitor olaparib.

物理化学性质&存储条件

分子量	525.686
分子式	C26H31N5O3S2
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	2-Propenamide, N-[4-[[(3R)-3-[[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]amino]-1-piperidinyl]carbonyl]phenyl]-

参考文献

1. Yao Liu, et al. J Med Chem. 2020 Jul 9;63(13):6708-6726.

MFH290 (MFH-290, MFH 290)

生物&药学活性

物理化学性质&存储条件

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MFH290 (MFH-290, MFH 290)

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物理化学性质&存储条件

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