FLAVOPIRIDOL HYDROCHLORIDE
FLAVOPIRIDOL HYDROCHLORIDE Basic information
- Product Name:
- FLAVOPIRIDOL HYDROCHLORIDE
- Synonyms:
-
- Flavopiridol hydrochloride, >=98%
- Alvocidib HCL
- Flavopiridol (Alvocidib) hydrochloride
- Flavopiridol hydrochloride hydrate
- NSC-649890 hydrochloride
- HL 275; NSC 649890; MDL 107826A; FLAVOPIRIDOL HCL; ALVOCIDIB HYDROCHLORIDE
- FLAVOPIRIDOL HYDROCHLORIDE
- FLAVOPIRIDOL HCL
- CAS:
- 131740-09-5
- MF:
- C21H21Cl2NO5
- MW:
- 438.3
- EINECS:
- 634-346-4
- Product Categories:
-
- Inhibitors
- Aromatics
- Chiral Reagents
- Heterocycles
- Intermediates & Fine Chemicals
- Pharmaceuticals
- Mol File:
- 131740-09-5.mol
FLAVOPIRIDOL HYDROCHLORIDE Chemical 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
- CAS DataBase Reference
- 131740-09-5
FLAVOPIRIDOL HYDROCHLORIDE Usage And Synthesis
Description
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.
Chemical Properties
Yellow Powder
Uses
An inhibitor of cyclin-dependent kinases; the (-)-cis form induces apoptosis in certain tumor cells.
Uses
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
Definition
ChEBI: A hydrochloride salt resulting from the formal reaction of equimolar amounts of alvocidib and hydrogen chloride. A cyclin-dependent kinase 9 (CDK9) inhibitor, it has been studied for the treatment of acute myeloid leukaemia, arthritis and atherosclerotic p aque formation.
Biochem/physiol Actions
Flavopiridol?is a semi-synthetic flavone obtained from Dysoxylum binectariferum that acts as an anti-tumor agent against several cancers. It also shows anti-cancer properties due to which it has been studied in the treatment of acute myeloid leukemia (AML).
storage
Store at +4°C
References
1) Kaur?et al. (1992),?Growth inhibition with reversible cell cycle arrest of carcinoma cells by flavone L86-8275;? J. Natl. Cancer Inst.,?84?1736 2) Cartee?et al. (2002),?Synergistic induction of apoptosis in human myeloid leukemia cells by phorbol 12-myristate 13-acetate and flavopiridol proceeds via activation of both the intrinsic and tumor necrosis factor-mediated extrinsic cell death pathways;? Mol. Pharmacol.,?61?1313 3) Ambrosini?et al. (2008),?The cyclin-dependent kinase inhibitor flavopiridol potentiates the effects of topoisomerase I poisons by suppressing Rad51 expression in a p53-dependent manner;? Cancer Res.?68?2312 4) Schang?et al. (2004),?Effects of pharmacological cyclin-dependent kinase inhibitors on viral transcription and replication;? Biochim. Biophys. Acta,?1697?197
FLAVOPIRIDOL HYDROCHLORIDESupplier
- Tel
- sales@boylechem.com
- Tel
- 010-82848833 400-666-7788
- jkinfo@jkchemical.com
- Tel
- +86-21-20908456
- sales@BioChemBest.com
- Tel
- 021-50135380
- shchemsky@sina.com
- Tel
- +86 (531) 88811783
- sales@trio-pharmatech.com (International market)
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