EPZ015666

EPZ015666 구조식 이미지
카스 번호:
1616391-65-1
상품명:
EPZ015666
동의어(영문):
CS-1657;EPZ015666;GSK3235025;GSK-3235025;EPZ015666 USP/EP/BP;EPZ-015666;EPZ 015666;GSK3235025 (EPZ015666);EPZ 015666 - GSK 3235025;EPZ-015666;EPZ 015666;GSK3235025;N-[(2S)-3-(3,4-Dihydro-2(1H)-isoquinolinyl)-2-hydroxypropyl]-6-(3-oxetanylamino)-4-pyrimidinecarboxamide
CBNumber:
CB02744609
분자식:
C20H25N5O3
포뮬러 무게:
383.44
MOL 파일:
1616391-65-1.mol

EPZ015666 속성

녹는점
124-131°C
끓는 점
686.4±55.0 °C(Predicted)
밀도
1.331±0.06 g/cm3(Predicted)
저장 조건
2-8°C
용해도
DMSO에 용해됨(최대 20mg/ml)
산도 계수 (pKa)
12.40±0.46(Predicted)
물리적 상태
가루
색상
흰색에서 베이지색
안정성
제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
CAS 데이터베이스
1616391-65-1

안전

EPZ015666 C화학적 특성, 용도, 생산

용도

Protein arginine methyltransferases (PRMTs) target nuclear and cytoplasmic substrates and can alter protein actions and gene expression. PRMT5, which can methylate histones H2A, H3, and H4, ribonucleoproteins, and other proteins, is upregulated in several human cancers, including lymphomas. Moreover, suppression of PRMT5 expression induces lymphoma cell death. EPZ015666 is a potent, orally bioavailable inhibitor of PRMT5 (Ki = 5 nM). It displays more than 20,000-fold selectivity for PRMT5 over other PMTs. EPZ015666 acts by blocking the association of PRMT5 with methylosome protein 50, which is necessary for the formation of an active methyltransferase complex. EPZ015666 (100 mg/kg twice daily) blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.[Cayman Chemical]

Biochem/physiol Actions

EPZ015666 (GSK3235025) is a protein arginine methyltransferase PRMT5 inhibitor with an IC50 value of of 22 nM in biochemical assays and no inhibition up to the maximum tested concentration of 50 μM against a panel of 20 other protein methyltransferases. Inhibition was uncompetitive with respect to SAM. EPZ015666 showed dose-dependent antitumor activity in multiple in vitro and in vivo mantle cell lymphoma (MCL) models with treatment of MCL cell lines leading to inhibition of SmD3 methylation and cell death.

EPZ015666 준비 용품 및 원자재

원자재

준비 용품


EPZ015666 공급 업체

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