Flavopiridol

Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively). It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM. Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model. It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.Formal Name: 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one. CAS Number: 146426-40-6. Synonyms: Alvocidib, HL 275, HMR 1275, L-868,275. Molecular Formula: C21H20ClNO5. Formula Weight: 401.8. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 5 mg/mL, DMSO: 30 mg/mL, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/mL, Ethanol: 3 mg/mL. lambdamax: 214, 272, 344 nm. SMILES: ClC1=C(C(OC2=C3C(O)=CC(O)=C2[C@H]4CCN(C)C[C@H]4O)=CC3=O)C=CC=C1. InChi Code: InChI=1S/C21H20ClNO5/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,17,24-25,27H,6-7,10H2,1H3/t12-,17+/m0/s1. InChi Key: BIIVYFLTOXDAOV-YVEFUNNKSA-N.