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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 |
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