Target Validation Information
TTD ID	T89361
Target Name	Cyclin-dependent kinase 6 (CDK6)
Type of Target	Successful
Drug Potency against Target	Flavopiridol	Drug Info	IC50 = 60 nM	[2]
	Palbociclib	Drug Info	Ki = 15 nM	[3]
	3,7,3',4'-TETRAHYDROXYFLAVONE	Drug Info	IC50 = 850 nM	[1]
	APIGENIN	Drug Info	IC50 = 1700 nM	[1]
	Chrysin	Drug Info	IC50 = 6000 nM	[1]
Action against Disease Model	Palbociclib	Drug Info	Inhibited cellular proliferation with IC50 = 40-400 nM in RB1-positive cell lines and IC50 > 3 mM in RB1-negative cell lines; induced G1 arrest in primary bone marrow myeloma cells and prevented t uMour growth in disseminated h uMan myeloma xenografts; promoted t uMour regression in mice with a h uMan colon carcinoma xenograft.	[2]
References
REF 1	Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005 Feb 10;48(3):737-43.
REF 2	Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
REF 3	Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004 Nov;3(11):1427-38.

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