KB-0742 is a potent, selective and orally active CDK9 inhibitor with an IC50 of 6 nM for CDK9/cyclin T1. KB-0742 is selective for CDK9/cyclin T1 with >50-fold selectivity over other CDK kinases. KB-0742 has potent anti-tumor activity[1].
in vivo
KB-0742 (3-30 mg/kg; p.o.; daily; over 21 days) is well tolerated even at high dose, while significantly reducing tumor burden in 22Rv1 human prostate cancer cell line-derived xenograft (CDX) models[1].
Animal Model:
Male CB17-SCID mice injected with 22Rv1 human prostate cancer cells[1]
Dosage:
3 mg/kg, 10 mg/kg, and 30 mg/kg
Administration:
p.o.; daily; over 21 days
Result:
Significantly reduced tumor growth in castration-resistant prostate cancer (CRPC).
IC 50
CDK9/cyclinT1: 6 nM (IC50)
References
[1] André Richters, et al. Modulating Androgen Receptor-Driven Transcription in Prostate Cancer with Selective CDK9 Inhibitors. Cell Chem Biol. 2020 Oct 20;S2451-9456(20)30380-9. DOI:10.1016/j.chembiol.2020.10.001
