IV-361

• CAT Number: I044457
• CAS Number: 2055741-39-2
• Molecular Formula: C23H32FN5O2Si
• Molecular Weight: 457.62
• Purity: ≥95%
• Synonyms: N-(5-fluoro-2-methylphenyl)-6,6-dimethyl-3-[(1-trimethylsilylcyclobutanecarbonyl)amino]-1,4-dihydropyrrolo[3,4-c]pyrazole-5-carboxamide
• InChI: InChI=1S/C23H32FN5O2Si/c1-14-8-9-15(24)12-17(14)25-21(31)29-13-16-18(22(29,2)3)27-28-19(16)26-20(30)23(10-7-11-23)32(4,5)6/h8-9,12H,7,10-11,13H2,1-6H3,(H,25,31)(H2,26,27,28,30)
• InChIKey: FYIUNJAFLWNBAI-UHFFFAOYSA-N
• SMILES: CC1=C(C=C(C=C1)F)NC(=O)N2CC3=C(C2(C)C)NN=C3NC(=O)C4(CCC4)[Si](C)(C)C

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].

Reference

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