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	CAS No.	Information
PC-62298	TPX 0005	1802220-02-5	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.
PC-45886	Crizotinib hydrochloride	1415560-69-8	Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.
PC-45885	Crizotinib	877399-52-5	Crizotinib (PF-02341066;PF-2341066) is a potent, selective, orally bioavailable, ATP-competitive inhibitor of c-Met catalytic activity with Ki of 4 nM.
PC-20033	Ficonalkib	2233574-95-1	Ficonalkib is a potent, selective anaplastic lymphoma kinase (ALK) inhibitor for treating an ALK-mediated disease.
PC-49613	TQ-B3139	1621519-26-3	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.
PC-73458	Zilurgisertib	2173389-57-4	Zilurgisertib is a potent, selective ALK 2 inhibitor with anti-cancer activity.
PC-73422	Iruplinalkib	1854943-32-0	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.

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