Pyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(5-fluoro-2-methylphenyl)-4,6-dihydro-6,6-dimethyl-3-[[[1-(trimethylsilyl)cyclobutyl]carbonyl]amino]-

Biological Activity

IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1)[1]. IV-361 has less inhibition on CDK2 (Ki≥1000 nM) or PLK1 (Ki≥5000 nM)[1]. IV-361 exhibits excellent IL-2 and IL-17 production inhibitory activity (all IC50≤100 nM) in periphery blood mononuclear cell (PBMC)[1]. IV-361 exhibits excellent HCT-116 cell growth inhibitory activity (GI50≤100 nM)[1]. IV-361 (25 mg/kg/day; orally) exhibits 46% or more rate of suppression of tumor volume in female BALB nude mice with HCT-116[1].

References

[1]. Noriaki Iwase, et al. Substituted dihydropyrrolopyrazole derivative. US20190256531A1.