SCH 529074

SCH 529074 구조식 이미지
카스 번호:
922150-11-6
상품명:
SCH 529074
동의어(영문):
SCH 529074;N3-[2-[[4-[Bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-1,3-propanediamine;N1-(2-((4-(Bis(4-chlorophenyl)methyl)piperazin-1-yl)methyl)quinazolin-4-yl)-N3,N3-dimethylpropane-1,3-diamine;1,3-Propanediamine, N3-[2-[[4-[bis(4-chlorophenyl)methyl]-1-piperazinyl]methyl]-4-quinazolinyl]-N1,N1-dimethyl-
CBNumber:
CB93146379
분자식:
C31H36Cl2N6
포뮬러 무게:
563.56
MOL 파일:
922150-11-6.mol

SCH 529074 속성

끓는 점
640.3±55.0 °C(Predicted)
밀도
1.262±0.06 g/cm3(Predicted)
저장 조건
Store at -20°C
용해도
DMF: 33 mg/ml; DMSO: 25 mg/ml; Ethanol: 33 mg/ml
물리적 상태
결정성 고체
산도 계수 (pKa)
9.44±0.28(Predicted)
색상
Off-white to light yellow

안전

SCH 529074 C화학적 특성, 용도, 생산

개요

SCH 529074 is a small molecule activator of p53, a tumor suppressor that is mutated or non-functional in 50% of human tumors. SCH 529074 restores DNA binding activity and increases DNA binding affinity of two recombinant GST fusion mutant p53 DNA binding domains (R273H and R249S) in an electrophoretic mobility shift assay with Kd values of 0.6740 and 0.4313, respectively. It also stimulates DNA binding activity and prevents human double minute-2 (Hdm-2) ubiquitination of wild-type p53 in vitro. SCH 29074 reduces proliferation of tumor cell lines with mutant and wild-type p53 (EC50s = 400-3,700 nM), with the p53 mutant cell lines being the most sensitive. In vivo, SCH 529074 reduces tumor growth in a DLD-1 human colorectal cancer xenograft model in mice in a dose-dependent manner.

용도

SCH 529074 is a small molecule activator of mutant p53, which binds p53 DNA binding domain (DBD), restores growth-suppressive function to mutant p53 and interrupts HDM2-mediated ubiquination of wild type p53.

SCH 529074 준비 용품 및 원자재

원자재

준비 용품


SCH 529074 공급 업체

글로벌( 43)공급 업체
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