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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-GFH009
GFH009

Chemical Structure : GFH009

CAS No.: 2247481-08-7

GFH009 (GFH 009)

货号: PC-21562Not For Human Use, Lab Use Only.

GFH009 is a potent, highly selective CDK9 inhibitor with IC50 of 9 nM against CDK9/Cyclin T1 complex, blocks RNAP2-mediated transcription maturation.

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纯度 & COA & 质检文件 纯度: 99.9% (HPLC) Select Batch:

生物&药学活性

GFH009 is a potent, highly selective CDK9 inhibitor with IC50 of 9 nM against CDK9/Cyclin T1 complex, blocks RNAP2-mediated transcription maturation.
shows negligible effects on other CDK family members
GFH009 demonstrates effective antiproliferative activity in a variety of human hematologic malignancy cell lines, with IC50 values below 0.2 μM in 7 of the 10 lines tested.
GFH009 demonstrates significant reduction of MCL-1 and proto-oncogene c-Myc, increases apoptosis markers Cleaved caspase-3 and Cleaved PARP in MV-4-11 cell cultures.
GFH009 (2.5 mg/kg-10 mg/kg, i.v.) exhibits tumor growth inhibition in MV-4-11 xenograft in female BALB/c nude mice.

物理化学性质&存储条件

分子量 519.11
分子式 C25H35ClN6O2S
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

4-[[[4-[5-Chloro-2-[[trans-4-[[(1R)-2-methoxy-1-methylethyl]amino]cyclohexyl]amino]-4-pyridinyl]-2-thiazolyl]amino]methyl]tetrahydro-2H-pyran-4-carbonitrile

参考文献

1. Zhou F, et al. Oncotarget. 2023 Dec 20;14:997-1008.

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