GFH009 | CDK9 inhibitor | Probechem Biochemicals

Chemical Structure : GFH009

CAS No.: 2247481-08-7

GFH009 (GFH 009)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	519.11
Formula	C25H35ClN6O2S
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

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

GFH009 (GFH 009)

Biological Activity

Physicochemical Properties

References

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