Entrectinib|1108743-60-7|(恩曲替尼; NMS-E628; RXDX-101)-陌孚医药/Medlife

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Entrectinib (Synonyms: 恩曲替尼; NMS-E628; RXDX-101)

目录号: PL12422 纯度: ≥99%

CAS No. :1108743-60-7

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中文名称	Entrectinib
中文别名	恩曲替尼;Entrectinib 抑制剂;Entrectinib（NMS-E628）抑制剂;N-(5-(3,5-二氟苄基)-1H-吲唑-3-基)-4-(4-甲基哌嗪-1-基)-2-(四氢-2H-吡喃-4-基氨基)苯甲酰胺
英文名称	Entrectinib
英文别名	N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-methylpiperazin-1-yl)-2-(tetrahydro-2H-pyran-4-ylamino)benzamide;Entrectinib;NMS-E628;RXDX-101;N-[5-[(3,5-Difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]benzamide;RXDX 101;Entrectinib(RXDX-101);L5ORF0AN1I;Benzamide, N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methyl-1-piperazinyl)-2-[(tetrahydro-2H-pyran-4-yl)amino]-;Benzamide, N-(5-((3,5-difluorophenyl)methyl)-1H-indazol-3-yl)-4-(4-methyl-1-piperazinyl)-2-((tetrahydro-2H-pyran-4-yl)amino)-;N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide;Entrectinib [USAN:INN];Rozlytrek;YMX;Entrectinib,;N-{5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-yl}-4-(4-methylpiperazin-1-yl)-2-[(oxan-4-yl)amino]benzamide;N-[5-[(3,5-difluorophenyl)methyl]-1H-indazol-3-
Cas No.	1108743-60-7
分子式	C₃₁H₃₄F₂N₆O₂
分子量	560.64
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Entrectinib (NMS-E628) 是有效，有口服活性的且具有中枢神经活性的 Trk, ROS1 和 ALK 抑制剂，抑制 TrkA, TrkB, TrkC, ROS1 和 ALK 的IC₅₀ 值分别为 1, 3, 5, 12 和 7 nM。具有抗肿瘤活性。

生物活性

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 IC 50 values of 1, 3, 5, 12 and 7 nM, respectively. Antitumor activity.

性状

Solid

IC50 & Target[1][2]

TrkA TrkB

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 (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

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. Single agent therapy results in significant tumor growth inhibition in animals treated with entrectinib compared to control animals. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : ≥ 31 mg/mL (55.29 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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