Flavopiridol Inhibitor CAS No. 146426-40-6

Cat. No.	Name	Size	Price
KI1223	Flavopiridol	10 mg	$176
	Flavopiridol	25 mg	$281.6
	Flavopiridol	50 mg	$486.4
	Flavopiridol	100 mg	$870.4
	Flavopiridol	200 mg	$1510.4

Chemical Characteristic

Product Name	Flavopiridol
Synonyms	Alvocidib, HMR-1275, L86-8275
CAS No.	146426-40-6
Molecular Weight	401.84
Formula	C₂₁H₂₀ClNO₅
Chemical Name	2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methylpiperidin-4-yl]chromen-4-one
Smiles	c1(cc(=O)c2c(cc(c(c2o1)C1[C@@H](CN(CC1)C)O)O)O)c1c(cccc1)Cl
Chemical Structure

Biological activities

Flavopiridol is a potent CDK inhibitor with IC50 values of 30, 170, 100, 170, 80 and 20 nM for CDK1, CDK2, CDK4, CDK5, CDK6 and CDK9, respectively. In a clonogenic assay, flavopiridol inhibits colony formation of PC-3 prostate carcinoma, PaCa-2 pancreatic carcinoma, HCT116 colorectal carcinoma and A2780 ovarian carcinoma cells with IC50 values of 10, 36, 13 and 15 nM, respectively.^[1]^[2] Flavopiridol treatment (150 and 300 nM) inhibits colony formation by 50% and 95%, respectively. In p21-intact Hct116 xenografts in vivo, mice treated with CPT-11 followed by flavopiridol (3 mg/kg) 7 and 16 hours later, tumor regression is by 86% and 82%, respectively, and the CR rates are 30% and 29%, respectively.^[3] In tumorigenic HNSCC cell line HN12 xenografts model in vivo, flavopiridol treatment (5 mg/kg) for 5 days leads to the appearance of apoptotic cells in the tumor xenografts and causes a 60-70% reduction in tumor size.^[4]

Protocols

In vivo: Flavopiridol is dissolved in DMSO.^[4]

References

[1] Kim KS, et al. Thio- and oxoflavopiridols, cyclin-dependent kinase 1-selective inhibitors: synthesis and biological effects. J Med Chem. 2000, 43(22): 4126-4134. [2] Lu H, et al. Crystal structure of a human cyclin-dependent kinase 6 complex with a flavonol inhibitor, fisetin. J Med Chem. 2005, 48(3): 737-743. [3] Motwani M, et al. Augmentation of apoptosis and tumor regression by flavopiridol in the presence of CPT-11 in Hct116 colon cancer monolayers and xenografts. Clin Cancer Res. 2001, 7(12): 4209-4219. [4] Patel V, et al. Flavopiridol, a novel cyclin-dependent kinase inhibitor, suppresses the growth of head and neck squamous cell carcinomas by inducing apoptosis. J Clin Invest. 1998, 102(9): 1674-1681.

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