貨號	規格	價格	上海	北京	武漢	南京
S80099-5mg	99.3%	￥125.00 S80099-5mg ￥125.00 現貨	4 4	-	-	-
S80099-10mg	99.3%	￥240.00 S80099-10mg ￥240.00 現貨	10 10	-	-	-
S80099-50mg	99.3%	￥800.00 S80099-50mg ￥800.00 現貨	7 7	-	-	-
S80099-100mg	99.3%	￥1250.00 S80099-100mg ￥1250.00 現貨	6 6	-	-	-
S80099-500mg	≥98%	￥3500.00 S80099-500mg ￥3500.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

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

產品描述：

靶點：

TrkA;TrkB;TrkC;Trkreceptor;ROS;ALK;Autophagy;ROSKinase

體外研究：

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

體內研究：

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

參考文獻：

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

保存條件：

-20℃

配置溶液濃度參考：

	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

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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