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• 产品描述： A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM[1]. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner

• 靶点： Mcl-1:0.45 nM (Ki);Bcl-2:132 nM (Ki);Bfl-1:660 nM (Ki);Bcl-W:2280 nM (Ki);Apoptosis;Apoptosis;BCL

• 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 IC50 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 IC50<10 μM, confirming that A-1210477 can kill MCL-1-dependent cell lines

• 参考文献：
  1. Leverson JD, et al. Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax). Cell Death Dis. 2015 Jan 15;6:e1590. 2. Qing Wang, et al. A-1210477, a selective MCL-1 inhibitor, overcomes ABT-737 resistance in AML. Oncol Lett. 2019 Nov;18(5):5481-5489.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.176 ml	5.882 ml	11.764 ml
  5 mM	0.235 ml	1.176 ml	2.353 ml
  10 mM	0.118 ml	0.588 ml	1.176 ml
  50 mM	0.024 ml	0.118 ml	0.235 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *