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Repotrectinib
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Repotrectinib图片
CAS NO:1802220-02-5
包装与价格：
包装价格(元)
5mg询价
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50mg询价

Repotrectinib (TPX-0005) 是一种有效的 ROS1 (IC50=0.07 nM) 和 TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) 抑制剂。 Repotrectinib 有效抑制 WT ALK (IC50=1.01 nM)。 Repotrectinib 具有抗癌活性。
Cas No.1802220-02-5
别名洛普替尼,TPX-0005
Canonical SMILESO=C1NC[C@H](C)OC2=CC=C(F)C=C2[C@@H](C)NC3=NC4=C1C=NN4C=C3
分子式C18H18FN5O2
分子量355.37
溶解度DMSO : ≥ 83.3 mg/mL (234.40 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM), TRK (0.83/0.05/0.1 nM=TRKA/B/C) inhibitor. Repotrectinib (TPX-0005) potently inhibits WT ALK (1.01 nM) and mutant ALKs including ALK G1202R (1.26 nM) and ALK L1196M (1.08 nM). It also inhibits a variety of other kinases, including JAK2, LYN, Src, and FAK (1.04, 1.66, 5.3, and 6.96 nM, respectively) [1][2].

Repotrectinib (TPX-0005) effectively overcomes this primary resistance (IC50 100 nM in cell proliferation assay) with strong inhibition of the phosphorylation of EML4-ALK (IC50 13 nM) and the SRC substrate paxillin (IC50 107 nM). Repotrectinib inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib[1].

Repotrectinib (TPX-0005) effectively inhibits tumor growth in vivo in ALK WT and ALK G1202R xenografts[1].

References:
[1]. Dayong Zhai, et al. Abstract 2132: The novel, rationally-designed, ALK/SRC inhibitor TPX-0005 overcomes multiple acquired resistance mechanisms to current ALK inhibitors. Cancer Research. July 2016
[2]. Karachaliou N, et al. Common Co-activation of AXL and CDCP1 in EGFR-mutation-positive Non-smallcell Lung Cancer Associated With Poor Prognosis. EBioMedicine. 2018 Mar;29:112-127.

 
 
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