• 产品描述： BRM/BRG1 ATP Inhibitor-1 (compound 14) is an orally active allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 µM. BRM/BRG1 ATP Inhibitor-1 has anticancer activity

• 靶点： IC50: ﹤0.005 µM (BRM, BRG1);EpigeneticReaderDomain

• 体外研究：
  BRM/BRG1 ATP Inhibitor-1 (compound 14) (0-10 μM，5 days) 可以抑制癌细胞的增殖。 BRM/BRG1 ATP Inhibitor-1 抑制 KRT80 基因的表达，在 H1299 细胞中的 AAC50 (绝对 AC50) 值为 0.01 μM，在 RERF-LC-AI 细胞中的 AAC50 为 0.01 μM。 Cell Proliferation Assay Cell Line: SKMEL5 melanoma cells and SBC-5 small cell carcinoma Concentration: 0-10 μM Incubation Time: 5 days Result: Inhibited the proliferation of SKMEL5 cells with an AAC50 (absolute AC50) value of 0.004 μM and of SBC-5 cells with the AAC50more than 10 μM.

• 体内研究：
  BRM/BRG1 ATP Inhibitor-1 (化合物14) (口服，7.5或20 mg/kg，每天，3周) 可抑制肿瘤生长，并呈剂量依赖性抑制KRT80表达。 Animal Model: Female athymic nude mice with RERF-LC-AI tumor xenografts Dosage: 7.5 mg/kg, 20 mg/kg Administration: Oral administration; everyday; 3 weeks Result: Inhibited tumor growth by 21% and 55% at doses of 7.5 mg/kg and 20 mg/kg, respectively.Inhibited KRT80 expression by up to 90% at 20 mg/kg for 7 hours after administration.

• 参考文献：
  1. Papillon JPN, et al. Discovery of Orally Active Inhibitors of Brahma Homolog (BRM)/SMARCA2 ATPase Activity for the Treatment of Brahma Related Gene 1 (BRG1)/SMARCA4-Mutant Cancers. J Med Chem. 2018 Nov 21;61(22):10155-10172

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.142 ml	15.71 ml	31.42 ml
  5 mM	0.628 ml	3.142 ml	6.284 ml
  10 mM	0.314 ml	1.571 ml	3.142 ml
  50 mM	0.063 ml	0.314 ml	0.628 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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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 *