CTX-439 (CTX439)

Chemical Structure : CTX-439

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货号: PC-26376Not For Human Use, Lab Use Only.

CTX-439 is a potent, selective, orally bioavailable, ATP-competitive CDK12/13 inhibitor with IC50 of 3.1/ 9.2 nM towards CDK12/Cyclin K and CDK13/Cyclin K, respectively, in cell-free assays.

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生物&药学活性

CTX-439 is a potent, selective, orally bioavailable, ATP-competitive CDK12/13 inhibitor with IC50 of 3.1/ 9.2 nM towards CDK12/Cyclin K and CDK13/Cyclin K, respectively, in cell-free assays.
CTX-439 possesses a highly specific inhibitory activity towards CDK12/13 compared to other members of the CDK family proteins, showing > 550-fold higher binding affinity and 20-fold higher inhibitory activity than the closest family member, CDK9.
CTX-439 shows high binding affinity towards CDK12 (Kd=0.38 nM).
CTX-439 downregulated p-S2, but neither phosphorylation of S5 (p-S5) nor phosphorylation of S7 (p-S7) in breast cancer cell line SUM149PT, reduced Serine 423 (S423) of CDK12 phosphorylation level in a dose-dependent manner.
CTX-439 possesses profound anti-tumor effects with IC50 of 100.5 nM against SUM149PT in cell-based assay, shows anti-tumor activity against a broad range of breast and ovarian cancer cell lines.
CTX-439 (15-30 mg/kg, p.o.) showed marked in vivo anti-tumor activity in nude mice bearing SUM149PT xenografts.

物理化学性质&存储条件

分子量	671.70
分子式	C30H32F3N9O4S
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	Butanamide, N-[5-(2-methoxy-5-pyrimidinyl)-2-pyrazinyl]-N-[trans-4-[[4-[5-(methylsulfonyl)-3-pyridinyl]-5-(trifluoromethyl)-2-pyrimidinyl]amino]cyclohexyl]-

参考文献

1. Hiroko Yamakawa, et al.

2. Kawahara S, et al. Mol Cancer Ther. 2026 Mar 12. doi: 10.1158/1535-7163.MCT-25-0954.

CTX-439 (CTX439)

生物&药学活性

物理化学性质&存储条件

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CTX-439 (CTX439)

生物&药学活性

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