BAY 87-2243

BAY 87-2243 구조식 이미지
카스 번호:
1227158-85-1
상품명:
BAY 87-2243
동의어(영문):
CS-1786;BAY 87-2243;BAY 87-2243 USP/EP/BP;BAY 87-2243 BAY87-2243;BAY87 2243;BAY 87 2243;BAY87-2243;Ferroptosis,inhibit,HIFs,HIF-PH,HIF/HIF Prolyl-Hydroxylase,Inhibitor,BAY 87-2243,BAY 872243,Hypoxia-inducible factors,BAY 87 2243;5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole;1-cyclopropyl-4-{4-[(5-methyl-3-{3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl}-1H-pyrazol-1-yl)methyl]pyridin-2-yl}piperazine;1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-piperazine;Piperazine, 1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-
CBNumber:
CB22681993
분자식:
C26H26F3N7O2
포뮬러 무게:
525.53
MOL 파일:
1227158-85-1.mol
MSDS 파일:
SDS

BAY 87-2243 속성

끓는 점
677.7±65.0 °C(Predicted)
밀도
1.47±0.1 g/cm3(Predicted)
저장 조건
RT
용해도
DMSO(최대 25mg/ml) 또는 에탄올(10mg/ml)에 용해됩니다.
산도 계수 (pKa)
8.43±0.27(Predicted)
물리적 상태
고체
물리적 상태
단단한 모양
색상
하얀색
안정성
제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 또는 에탄올 용액은 -20°에서 최대 2개월 동안 보관할 수 있습니다.

안전

BAY 87-2243 C화학적 특성, 용도, 생산

효소 저해제

This Hif1a inhibitor (FW = 525.53 g/mol; CAS 1227158-85-1; Solubility: <1 mg/mL DMSO or H2O) targets the transcription factor hypoxia-inducible factor-1 (HIF-1), which plays an essential role in tumor development, tumor progression, and resistance to chemo- and radiotherapy. BAY 87-2243 inhibits HIF-1α and HIF-2α accumulation under hypoxic conditions in the H460 Non-Small Cell Lung Cancer (NSCLC) cell line but is without effect on HIF-1α protein levels that are induced by such hypoxia mimetics asdesferrioxamine or cobalt chloride. BAY 87-2243 has no effect on HIF target gene expression levels in RCC4 cells lacking Von Hippel-Lindau (VHL) activity; nor does it affect the activity of HIF prolyl hydroxylase-2. Antitumor activity of BAY 87-2243, suppression of HIF-1α protein levels, and reduction of HIF-1 target gene expression in vivo have been demonstrated in a H460 xenograft model. BAY 87-2243 does not inhibit cell proliferation under standard conditions. Upon glucose depletion, a condition favoring mitochondrial ATP generation as energy source, BAY 87-2243 inhibits cell proliferation in the low-nM range. In a mouse model for BRAF mutant melanoma, BAY 87-2243-mediated complex I inhibition induces melanoma cell death in vitro and reduces melanoma tumor growth in various mouse models in vivo. This effect is mediated through BAY 87-2243- induced stimulation of mitochondrial ROS production, leading to oxidative damage and subsequent cell death. BAY 87-2243 displays increased anti tumor efficacy compared to single agent treatment, when combined with the BRAF inhibitor vemurafenib in nude mice with BRAF mutant melanoma xenografts.

BAY 87-2243 준비 용품 및 원자재

원자재

준비 용품


BAY 87-2243 공급 업체

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ATK CHEMICAL COMPANY LIMITED
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InvivoChem
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ShenZhen Trendseen Biological Technology Co.,Ltd.
13417589054
trendseenbio@gmail.com China 11681 58
Wuhan Topule Biopharmaceutical Co., Ltd
+8618327326525
masar@topule.com China 8467 58

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