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S81382

MI-136

源叶(MedMol) ≥98%
  • 英文名:
  • 5-((4-((6-(2,2,2-trifluoroethyl)thieno[2,3-d]pyrimidin-4-yl)amino)piperidin-1-yl)methyl)-1H-indole-2-carbonitrile
  • 别名:
  • MI-136; MI136; MI 136
  • CAS号:
  • 1628316-74-4
  • 分子式:
  • C23H21F3N6S
  • 分子量:
  • 470.5132
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81382-5mg ≥98% ¥989.00元 10 - - - EA 加入购物车
源叶(MedMol) S81382-10mg ≥98% ¥1700.00元 10 - - - EA 加入购物车
源叶(MedMol) S81382-25mg ≥98% ¥3398.00元 9 - - - EA 加入购物车
源叶(MedMol) S81382-50mg ≥98% ¥5350.00元 5 - - - EA 加入购物车
源叶(MedMol) S81382-100mg ≥98% ¥9681.00元 6 - - - EA 加入购物车
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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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