FlavopiridolHydrochloride , 98% , 131740-09-5

Synonym(s):
(−)-2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]-4H-1-benzopyran-4-one hydrochloride;L-86-8276;NSC-649890

CAS NO.：131740-09-5

Empirical Formula: C21H21Cl2NO5

Molecular Weight: 438.3

MDL number: MFCD26792554

EINECS: 634-346-4

PRODUCT Properties

• Melting point: 169.5-170°C
• alpha: 24D -1.73 to -3.9°
• storage temp.: 2-8°C
• solubility: H2O: ~2mg/mL
• form: powder
• pka: 5.68 ± 0.06(at 25℃)
• color: white to light brown
• Stability: Stable for 2 years from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 1 month

Description and Uses

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 K_i 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 HEK239T cells (IC₅₀ = <10 nM). 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.

Flavopiridol hydrochloride hydrate has been used:

• as a cyclin-dependent kinase 9 (CDK9) inhibitor to study its effects on histone H3 methylation at lysine 36 (H3K36) and deactivation of transcription in porcine fetal fibroblasts
• as an RNA polymerase inhibitor to study its effects on hepatic cells
• as RNA transcription inhibitor to study its effects on euchromatin coarsening in zebrafish embryo

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338
• Hazard Codes: Xn
• Risk Statements: 22
• WGK Germany: 3
• RTECS: DJ2978830