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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-21788

Ensartinib

ALK inhibitor

Ensartinib (X-396) is a potent, selective and second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with biochemical IC50 of <0.4 nM, inhibits MET with IC50 of 0.74 nM.
PC-21774

Ceritinib

ALK inhibitor

Ceritinib (LDK378) is a potent, selective and orally active anaplastic lymphoma kinase (ALK) inhibitor with enzymatic IC50 of 200 pM, overcomes crizotinib resistance in NSCLC.
PC-20952

Unecritinib

ALK inhibitor

Unecritinib (TQ-B3101) is a novel kinase inhibitor targeting receptor tyrosine kinases including ALK, ROS1 and MET.
PC-20623

CEP-37440

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.
PC-20033

Ficonalkib

ALK inhibitor

Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease.
PC-73458

Zilurgisertib

ALK2 inhibitor

Zilurgisertib is a potent, selective ALK 2 inhibitor with anti-cancer activity.
PC-73422

Iruplinalkib

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.
PC-72134

ALK2 R206H inhibitor 23

ALK2 R206H inhibitor

ALK2 R206H inhibitor 23 is a potent and selective inhibitor of Activin Receptor-Like Kinase-2 (ALK2/ACVR1) with IC50 of 8 nM for mutant ALK2 R206H.
PC-72014

M4K2234

ALK1/2 inhibitor

M4K2234 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 7 and 14 nM, respectively.
PC-72012

MU1700

ALK1/2 inhibitor

MU1700 is a potent, selective ALK1 (ACVRL1) and ALK2 (ACVR1) protein kinase inhibitor with IC50 of 13 and 6 nM, respectively.
PC-35352

JH-VIII-157-02

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).
PC-35262

WY-135

WY-135 (WY135) is a novel potent inhibitor of ALK and ROS1 with IC50 of 1.2 and 0.48 nM, respectively.

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