中文同义词:
7-[5-[[4-[4-[(二甲基氨基)磺酰基]-1-哌嗪基]苯氧基]甲基]-1,3-二甲基-1H-吡唑-4-基]-1-[2-(4-吗啉基)乙基]-3-[3-(1-萘基氧基)丙基]-1H-吲哚-2-羧酸;MCL-1抑制剂(A-1210477);BIIB-024, TAK580, AMG-2112819, BSK1369, DAY-101
英文同义词:
A-1210477;7-(5-((4-(4-(N,N-dimethylsulfamoyl)piperazin-1-yl)phenoxy)methyl)-1,3-dimethyl-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid;Abbvie Mcl-1 Inhibitor;7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid;CS-2202;CS-2151;A-1210477;A 1210477;A1210477;1H-Indole-2-carboxylic acid, 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-
相关类别:
小分子抑制剂;小分子抑制剂，天然产物;抑制剂;细胞生物学试剂;Inhibitors
沸点
1027.4±65.0 °C(Predicted)
密度
1.32±0.1 g/cm3(Predicted)
储存条件
Sealed in dry,Store in freezer, under -20°C
酸度系数(pKa)
4.43±0.30(Predicted)
生物活性
A-1210477 是一种有效，选择性的 MCL-1 抑制剂，Ki 值为 0.45 nM。A-1210477 特异性结合 MCL-1，并以 MCL-1 依赖性方式促进癌细胞凋亡 (apoptosis)。
靶点
Mcl-1
0.45 nM (Ki)
Bcl-2
132 nM (Ki)
Bfl-1
660 nM (Ki)
Bcl-W
2280 nM (Ki)
Apoptosis
Mcl-1
0.45 nM (Ki)
Bcl-2
132 nM (Ki)
体外研究
A-1210477 (10 μM) reduces the amount of BIM co-immunoprecipitated with MCL-1 antibody, and triggers MCL-1 elevation in a variety of cancer cell lines, including the breast cancer cell line HCC-1806. A-1210477 inhibits MCL-1-NOXA interactions with an IC 50 of approximately 1 μM, while having no effect on BCL-2-BIM or BCL-XL-BCL-XS interactions. The NSCLC cell lines H2110 and H23 are sensitive to A-1210477 with cell viability IC 50 <10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines.
