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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.


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


FAK/ALK inhibitor

CEP-37440 (CEP37440) is a potent, selective, and brain penetrant dual FAK/ALK inhibitor with IC50 of 2.0/3.1 nM, respectively.


ALK inhibitor

Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease.


ALK/c-MET inhibitor

TQ-B3139 (Envonalkib, CT-711) is a potent inhibitor of ALK and c-Met kinases with IC50 of 14.3 and 12.5 nM in cell-free assays, respectively.


ALK2 inhibitor

Zilurgisertib (INCB000928, NBU-928) is a potent, selective and orally available wild-type and mutant ALK2 (R206H).


ALK inhibitor

Iruplinalkib (WX-0593) is a potent ALK inhibitor, inhibits the activity of both wild type (IC50=5.38 nM) and resistant mutants of ALK (ALKL1196M IC50=9.26 nM) in vitro, and overcomes crizotinib-resistant mutations.


ALK inhibitor

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).


ALK1/2 inhibitor

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.


ALK1/2 inhibitor

MU1700 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 13 and 6 nM, respectively.


ALK inhibitor

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.


ALK5 inhibitor

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.


ALK G1202R inhibitor

JH-VIII-157-02 is a potent, orally active, CNS-permeable, second-generation inhibitor of ALK G1202R mutant with IC50 of 2 nM, also shows high potency against a variety of other frequently observed mutants (G1269A, S1206Y, F1174L and C1156Y).


ALK inhibitor

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.

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