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S80285

Dubermatinib

源叶(MedMol) 98%
  • 英文名:
  • TP-0903
  • 别名:
  • TP0903
  • CAS号:
  • 1341200-45-0
  • 分子式:
  • C24H30ClN7O2S
  • 分子量:
  • 516.0587
  • 核磁/质谱:
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) S80285-5mg 98% ¥530.00元 6 - - - EA 加入购物车
源叶(MedMol) S80285-10mg 98% ¥850.00元 6 - - - EA 加入购物车
源叶(MedMol) S80285-25mg 98% ¥1700.00元 6 - - - EA 加入购物车
源叶(MedMol) S80285-100mg 98% ¥5100.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: TP-0903 is a potent and selective Axl kinase inhibitor.
  • 靶点: Apoptosis;TAM Receptor;Apoptosis;TAMReceptor
  • 体外研究:
    In pancreatic cancer cells (PSN-1), TP-0903 shows strong antiproliferative activity with IC50 of 6 M. TP-0903 also induces strong G2/M arrest by potently inhibiting Aurora A and B. In CLL B cells from all the patients with CLL, TP-0903 causes a dose-dependent induction of massive apoptosis by targeting phosphorylated Axl, and overcomes CLL BMSC-mediated protection of CLL B cells from apoptosis.
  • 体内研究:
    In the adult rat hippocampus, the intracerebroventricular administration of SAG (2.5 nM) significantly increases the number of newly generated cells and extends survival of hippocampal cells. [3] In mice, SAG (20 μg/g, i.p.) effectively prevents GC-induced neonatal cerebellar developmental abnormalities.
  • 细胞实验: For cell proliferation assays, 45 μL containing 1000 cells per well are seeded into solid white 384-well plates in appropriate media. The following day, TP-0903 is diluted in serum free growth media to 10x desired concentrations and 5 μL is added to each well. Combined compound and cells are incubated for 96 hours. Following incubation, 40 μL of ATP-Lite solution is added to each well, incubated for an additional 10 minutes at room temperature and luminescence is measured on an microplate reader
  • 参考文献:
    1. Mollard A, Warner SL, Call LT, Wade ML, Bearss JJ, Verma A, Sharma S, Vankayalapati H, Bearss DJ. Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors. ACS Med Chem Lett. 2011 Dec 8;2(12):907-912. 2. Sinha S, et al. Targeted Axl Inhibition Primes Chronic Lymphocytic Leukemia B Cells to Apoptosis and Shows Synergistic/Additive Effects in Combination with BTK Inhibitors. Clin Cancer Res. 2015, 21(9), 2115-2126.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.938 ml 9.689 ml 19.378 ml
    5 mM 0.388 ml 1.938 ml 3.876 ml
    10 mM 0.194 ml 0.969 ml 1.938 ml
    50 mM 0.039 ml 0.194 ml 0.388 ml
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