フラボピリドール塩酸塩 化学特性,用途語,生産方法
効能
抗悪性腫瘍薬, サイクリン依存性キナーゼ(CDK)阻害薬
説明
Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC
50s = ~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 (IC
50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC
50 = 7 nM), and HIV-1 replication in HEK239T cells (IC
50 = <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.
化学的特性
Yellow Powder
使用
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
定義
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.
フラボピリドール塩酸塩 上流と下流の製品情報
原材料
準備製品