CAS NO: | 1108743-60-7 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | Entrectinib (NMS-E628) is a potent, orally available, and CNS-activepan-Trk,ROS1, andALKinhibitor. Entrectinib inhibitsTrkA,TrkB,TrkC, ROS1 and ALK withIC50values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | 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 (IC50of 17 nM), the ALK-dependent ALCL cell lines SU-DHL-1, Karpas-299, SUP-M2 and SR-786 (IC50of 20, 31, 41, and 81 nM, respectively), the ALK-dependent NSCLC cell line NCI-H2228 (IC50of 68 nM) and the FLT3-dependent AML cell line MV-4-11 (IC50of 81 nM). Entrectinib potently blocks proliferation of Ba/F3-TEL-TRKB (IC50of 2.9 nM), Ba/F3-TEL-TRKC (IC50of 3.3 nM), and Ba/F3-TEL-ROS1 (IC50of 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[1]. Entrectinib significantly inhibits the growth of TrkB-expressing NB cellsin vitro, and it significantly enhances the growth inhibition of Irino-TMZ when used in combination[2]. | ||||||||||||||||
体内研究 (In Vivo) | 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[1]. Single agent therapy results in significant tumor growth inhibition in animals treated with entrectinib compared to control animals[2]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 560.64 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C31H34F2N6O2 | ||||||||||||||||
CAS 号 | 1108743-60-7 | ||||||||||||||||
中文名称 | 恩曲替尼 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : ≥ 31 mg/mL(55.29 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百
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