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Anaplastic lymphoma kinase (ALK), also known as CD246, is a receptor tyrosine kinase having a putative transmembrane domain and an extracellular domain. ALK activation is involved in the carcinogenesis process of several human cancers such as anaplastic large cell lymphoma, lung cancer, inflammatory myofibroblastic tumors and neuroblastoma, as a consequence of fusion with other oncogenes (NPM, EML4, TIM, etc) or gene amplification, mutation or protein overexpression.

Specific inhibitors, such as crizotinib, ceritinib, alectinib etc., has demonstrated significant effectiveness in ALK-positive patients, in particular ALK-positive non- small cell lung cancer. The EML4-ALK fusion gene is responsible for approximately 3-5% of non-small-cell lung cancer(NSCLC). The vast majority of cases are adenocarcinomas. Crizotinib is a first-in-class ALK tyrosine kinase inhibitor (TKI), which has proven its superiority over standard platinum-based chemotherapy for the first-line therapy of ALK-rearranged non-small cell lung cancer (NSCLC) patients. Ceritinib and alectinib are approved second-generation ALK TKIs. Several novel ALK inhibitors, more potent and with different selectivity compared to crizotinib, are currently in development.

References:

1. Della Corte CM, et al. Mol Cancer. 2018 Feb 19;17(1):30.

2. Wu W, et al. Cancers (Basel). 2017 Nov 30;9(12). pii: E164.

3. Muller IB, et al. Onco Targets Ther. 2017 Sep 13;10:4535-4541.

4. Karachaliou N, et al. Expert Opin Investig Drugs. 2017 Jun;26(6):713-722.

 

Cat. No. Product Name Information
PC-72509

TPX-0131

TPX-0131 (Zotizalkib, TPX0131) is a potent, CNS-penetrant, next-generation inhibitor of wild-type ALK (IC50=1.4 nM) and 26 ALK resistance mutations (all IC50=<1-7 nM).
PC-38244

XMU-MP-5

XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R.
PC-38197

THRX-144644

THRX-144644 (THRX144644) is a potent, lung-selective ALK5 inhibitor with IC50 of 0.14 nM, inhibits p-SMAD3 in a BEAS2B cell line with IC50 of 23 nM.
PC-43495

ASP3026

ASP3026 is a potent small molecule ALK inhibitor with IC50 of 3.5, 10, 5.4 and 6.8 nM for wt ALK, ALK F1174L, ALK R1275Q and NPM1-ALK, respectively.
PC-43260

Brigatinib

Brigatinib (AP-26113, AP26113) is a potent, selective, second generation ALK inhibitor with IC50 of 0.62 nM, exhibits about fivefold greater potency in vitro compared with crizotinib.
PC-42884

LDN193189

LDN193189 is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM).
PC-62298

TPX 0005

TPX 0005 (Ropotrectinib) is a novel ALK/ROS1/TRK inhibitor, effectively inhibits a broad spectrum of mutations including solvent front ALK G1202R, ROS1 G2032R and TRKA G595R mutants.

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