CDK6/9-IN-1

Names

[ Name ]:
CDK6/9-IN-1

Biological Activity

[Description]:

CDK6/9-IN-1 (compound 66) is an oral available and dual CDK 6 and CDK 9 inhibitor, with IC50 values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> CDK

[Target]

CDK6:40.5 nM (IC50)

CDK9:39.5 nM (IC50)

[In Vitro]

CDK6/9-IN-1 (compound 66, 4 or 8 μM in MDA-MB-231 cells) treatment induces G0/G1 cell cycle arrest (71.85% and 77.51%, respectively), when compared with the control (57.65%)[1].

[In Vivo]

CDK6/9-IN-1 (compound 66) significantly inhibits tumor growth in an xenograft mouse model with no obvious toxicity, indicating the promising therapeutic potential of CDK6/9 dual inhibitors for cancer treatment[1].

[References]

[1]. Yang Wang, et al. Discovery and SARs of 5-Chloro- N4-phenyl- N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors With Potent Antitumor Activity. J Med Chem. 2020 Mar 26;63(6):3327-3347.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₂H₂₅ClN₈O

[ Molecular Weight ]:
452.94

CDK6/9-IN-1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds