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IV-361

Names

[ CAS No. ]:
2055741-39-2

[ Name ]:
IV-361

Biological Activity

[Description]:

IV-361 is an orally active and selective CDK7 inhibitor (Ki≤50 nM). IV-361 has anti-cancer activity (US20190256531A1)[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

[Target]

CDK7:≤50 nM (Ki)

CDK2:≥1000 nM (Ki)


[In Vitro]

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].

[In Vivo]

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.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H32FN5O2Si

[ Molecular Weight ]:
457.62


Related Compounds