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
Pack Size | Price | Stock | Quantity |
5mg | RMB125.60 | In Stock |
|
10mg | RMB200.80 | In Stock |
|
50mg | RMB646.40 | In Stock |
|
100mg | RMB1033.60 | In Stock |
|
others | Enquire |
PRODUCT Properties
Melting point: | 169.5-170°C |
alpha | 24D -1.73 to -3.9° |
storage temp. | 2-8°C |
solubility | H2O: ~2mg/mL |
pka | 5.68 ± 0.06(at 25℃) |
form | powder |
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 |
CAS DataBase Reference | 131740-09-5 |
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 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 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 |