P276

P276 구조식 이미지
카스 번호:
920113-03-7
상품명:
P276
동의어(영문):
P276;CS-996;P276 USP/EP/BP;Riviciclib HCl;Riviciclib HCl (P276-00);Riviciclib hydrochloride;RIVICICLIB HYDROCHLORIDE (P276-00);inhibit,Inhibitor,Riviciclib,CDK,Riviciclib hydrochloride,Cyclin dependent kinase,Apoptosis;2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one:hydrochloride;2-(2-chlorophenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one hydrochloride
CBNumber:
CB32668296
분자식:
C21H21Cl2NO5
포뮬러 무게:
438.3
MOL 파일:
920113-03-7.mol

P276 속성

저장 조건
Store at -20° C
용해도
DMSO에 용해됨
물리적 상태
Solid
색상
Off-white to light yellow

안전

P276 C화학적 특성, 용도, 생산

용도

P276-00 is a cyclin-dependent kinase (CDK) inhibitor. P276-00 has shown to be highly selective for cancer cells and has shown to produce potent inhibition of Cdk4-D1 activity. P276-00 also induces apoptosis in human promyelocytic leukemia (HL-60) cells.

효소 저해제

This cell cycle-inhibiting flavone and anticancer agent (FW = 438.30 g/mol; CAS 920113-03-7), also named 2-(2-chlorophenyl)-5,7-dihydroxy-8- [(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4- one, targets the Cyclin-Dependent Kinases CDK1 (IC50 = 79 nM), CDK4 (IC50 = 63 nM) and CDK9 (IC50 = 20 nM). p276-00 showed potent antiproliferative effects against various human cancer cell lines (IC50 values ranging from 300 to 800 nmol/L), but has little effect on cultured fibroblasts. A significant down-regulation of cyclin D1 and Cdk4 and a decrease in Cdk4-specific pRb Ser(780) phosphorylation is observed. P276-00 produces potent inhibition of Cdk4-D1 activity that is competitive with ATP, and not with retinoblastoma protein. The compound also induced apoptosis in human promyelocytic leukemia (HL-60) cells, as evidenced by the induction of caspase-3 and DNA ladder studies. In 22 human cancer xenografts, P276-00 is approximately 26x more potent than cisplatin, and is also active against cisplatin-resistant tumors of central nervous system, melanoma, prostate, and renal cancers. Synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells are arrested in G1

P276 준비 용품 및 원자재

원자재

준비 용품


P276 공급 업체

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