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S80099

Entrectinib

源叶(MedMol) 98%
  • 英文名:
  • Entrectinib
  • 别名:
  • N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide; NMS E628; Entrectinib (RXDX-101); RXDX-101; RXDX101; NMS-E628; Entrectinib; RXDX 101
  • CAS号:
  • 1108743-60-7
  • 分子式:
  • C31H34F2N6O2
  • 分子量:
  • 560.6375
  • 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) S80099-5mg 98% ¥442.00元 6 - - - EA 加入购物车
源叶(MedMol) S80099-10mg 98% ¥680.00元 10 - - - EA 加入购物车
源叶(MedMol) S80099-50mg 98% ¥2176.00元 7 - - - EA 加入购物车
源叶(MedMol) S80099-100mg 98% ¥3672.00元 6 - - - EA 加入购物车
源叶(MedMol) S80099-500mg 98% ¥6664.00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: Entrectinib (NMS-E628) is a potent, orally available, and CNS-active pan-Trk, ROS1, and ALK inhibitor. Entrectinib inhibits TrkA, TrkB, TrkC, ROS1 and ALK with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity
  • 靶点: TrkA;TrkB;TrkC;Trkreceptor;ROS;ALK;Autophagy;ROSKinase
  • 体外研究:
    Entrectinib (NMS-E628) is found to be exquisitely active in inhibiting the proliferation of a limited number of cell lines: the TRKA-driven colorectal carcinoma cell line KM12 (IC50 of 17 nM), the ALK-dependent ALCL cell lines SU-DHL-1, Karpas-299, SUP-M2 and SR-786 (IC50 of 20, 31, 41, and 81 nM, respectively), the ALK-dependent NSCLC cell line NCI-H2228 (IC50 of 68 nM) and the FLT3-dependent AML cell line MV-4-11 (IC50 of 81 nM). Entrectinib potently blocks proliferation of Ba/F3-TEL-TRKB (IC50 of 2.9 nM), Ba/F3-TEL-TRKC (IC50 of 3.3 nM), and Ba/F3-TEL-ROS1 (IC50 of 5.3 nM) cells, with a high degree of selectivity versus parental Ba/F3 cells or those transformed by nontargeted kinases such as ABL and RET, which are inhibited with IC50s in the range of 2 to 3 μM. Entrectinib significantly inhibits the growth of TrkB-expressing NB cells in vitro, and it significantly enhances the growth inhibition of Irino-TMZ when used in combination
  • 体内研究:
    Oral administration of entrectinib to tumor-bearing mice induces regression in relevant human xenograft tumors, including the TRKA-dependent colorectal carcinoma KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including a model of brain-localized lung cancer metastasis. Single agent therapy results in significant tumor growth inhibition in animals treated with entrectinib compared to control animals
  • 参考文献:
    1. Ardini E, et al. Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications. Mol Cancer Ther. 2016 Apr;15(4):628-39. 2. Iyer R, et al. Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model. Cancer Lett. 2016 Mar 28;372(2):179-86.
  • 溶解性: soluble  in  DMSO
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.784 ml 8.918 ml 17.837 ml
    5 mM 0.357 ml 1.784 ml 3.567 ml
    10 mM 0.178 ml 0.892 ml 1.784 ml
    50 mM 0.036 ml 0.178 ml 0.357 ml
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