Anaplastic Lymphoma Kinase (ALK) (inhibitors, antagonists, agonists)-ProbeChem.com

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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-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.
PC-43330	GSK1838705A	GSK1838705A is a potent, specific inhibitor of IGF-IR and insulin receptor (IR) with IC50 of 2.0 and 1.6 nM, also is a potent inhibitor of ALK with IC50 of 0.5 nM.
PC-42979	KRCA-0008	KRCA-0008 is a potent, selective ALK inhibitor with IC50 of 12 nM (wt ALK), also is potent against various ALK mutants, including L1196M, F1174L, R1275Q, and C1156Y (IC50=5-75 nM).
PC-43321	Alectinib hydrochloride	A potent, selective ALK inhibitor with IC50 of 1.9 nM.
PC-42919	Lorlatinib	A novel CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively.
PC-45405	CEP-28122 mesylate	A highly potent and selective, orally active ALK inhibitor with IC50 of 1.9 nM.
PC-45404	CEP-28122	A highly potent and selective, orally active ALK inhibitor with IC50 of 1.9 nM.

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