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• 产品描述： MI-136 inhibits expression of androgen receptor (AR) target genes that DHT induced

• 靶点： Androgen Receptor;Apoptosis;Epigenetic Reader Domain;Apoptosis; EpigeneticReaderDomain; AndrogenReceptor

• 体外研究：
  MI-136, a variant of a previously described inhibitor that can specifically inhibit the menin-MLL interaction. AR positive cell lines such as VCaP, LNCaP and 22RV1 are sensitive to MI-136. Treatment with MI-136 also inhibits the expression of genes that are bound to ASH2L after AR stimulation. Treatment with MI-136 induces apoptosis of VCaP cells as evidenced by PARP (cPARP) cleavage and blocks DHT-induced cell proliferation in AR-dependent cell lines (LNCaP and VCaP). The effect of MI-136 on cell proliferation is similar to MDV-3100, a second-generation FDA-approved anti-androgen for patients with refractory prostate cancer.

• 体内研究：
  Treatment of VCaP tumor-bearing mice with MI-136 (40 mg/kg) leads to a modest but significant reduction in tumor volume with no effect on mouse body weight.

• 细胞实验： To assess the effect of MI-136 on AR signaling, VCaP cells are treated with DMSO or 5 μM MI-136 for 48 hours. Cells are serum starved by replacing the media with DMEM containing 5% charcoal-striped serum and MI-136 for 48 hrs. Cells are then stimulated with 10nM DHT for 12 hrs and RNA is isolated and processed for expression microarrays. (Only for Reference)

• 参考文献：
  1. Malik R, et al. Targeting the MLL complex in castration-resistant prostate cancer. Nat Med. 2015, 21(4):344-352.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.125 ml	10.627 ml	21.253 ml
  5 mM	0.425 ml	2.125 ml	4.251 ml
  10 mM	0.213 ml	1.063 ml	2.125 ml
  50 mM	0.043 ml	0.213 ml	0.425 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 *