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-23342	NVL-655 ALK inhibitor	Neladalkib (NVL-655) is a potent, selective and brain-penetrant fourth-generation inhibitor of diverse ALK-mutant oncoproteins with IC50 of 0.9 nM and 1.8 nM for WT ALK and ALK G1202R/L1196M mutant respectively.
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 (SY-3505) is a potent, selective, 3rd-generation anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 1.3 nM and 1.5 nM for WT ALK, and F1174L mutant.
PC-49613	TQ-B3139 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.
PC-73458	Zilurgisertib ALK2 inhibitor	Zilurgisertib (INCB000928, NBU-928) is a potent, selective and orally available wild-type and mutant ALK2 (R206H).
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-72509	TPX-0131 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).
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-38244	XMU-MP-5 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.
PC-38197	THRX-144644 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.

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