OKI-1546 | CDK12/13 inhibitor | Probechem Biochemicals

Chemical Structure : OKI-1546

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OKI-1546 (OKI1546, OKI 1546)

货号: PC-28533Not For Human Use, Lab Use Only.

OKI-1546 is a potent, selective, covalent and orally bioavailable CDK12/13 inhibitor with IC50 of 15 nM (CDK12), shows 649-, 81-, 11-, and 64-fold selective over CDKs 1, 2, 7, and 9, respectively.

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生物&药学活性

OKI-1546 is a potent, selective, covalent and orally bioavailable CDK12/13 inhibitor with IC50 of 15 nM (CDK12), shows 649-, 81-, 11-, and 64-fold selective over CDKs 1, 2, 7, and 9, respectively.
OKI-1546 potently inhibits proliferation of multiple cancer cell lines, with IC50 values that correlated with 50% inhibition of CTD pSer2.
OKI-1546 exhibits tumor growth inhibition in the BRCA1-mutant MDA-MB-436 tumor model in mice.
OKI-1546 induces a BRCAness phenotype and synergizes with merestinib in neuroblastoma (NB) cells and in vivo.

物理化学性质&存储条件

分子量	431.42
分子式	C21H20F3N5O2
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)-1-(5-(3-((5-(trifluoromethyl)pyrimidin-2-yl)amino)pyrrolidine-1-carbonyl)isoindolin-2-yl)prop-2-en-1-one

参考文献

1. Goulding JR, et al. Cell Rep. 2026 Oct 12;45(10):117997.

2. Alexander A. Strait, et al. Cancer Res (2023) 83 (7_Supplement): 1635.

OKI-1546 (OKI1546, OKI 1546)

生物&药学活性

物理化学性质&存储条件

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OKI-1546 (OKI1546, OKI 1546)

生物&药学活性

物理化学性质&存储条件

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