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-35352	JH-VIII-157-02 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).
PC-43495	ASP3026 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.
PC-43260	Brigatinib ALK inhibitor	Brigatinib (AP-26113, AP26113) is a potent, selective, second generation ALK inhibitor with IC50 of 0.62 nM, exhibits about fivefold greater potency in vitro compared with crizotinib.
PC-42979	KRCA-0008 ALK inhibitor	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-42885	LDN193189 hydrochloride ALK2/ALK3 inhibitor	LDN193189 is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM).
PC-42884	LDN193189 ALK2/ALK3 inhibitor	LDN193189 (DM 3189) is a potent, selective BMP type I receptor that inhibits BMP4-induced phosphorylation of SMAD1/5/8 with IC50 of 5 nM, displays >200-fold selectivity for BMP signaling over TGF-β signaling (IC50>1,000 nM).
PC-62298	Repotrectinib ALK/ROS1/TRK inhibitor	Repotrectinib (TPX-0005) 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	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-43321	Alectinib hydrochloride ALK inhibitor	Alectinib (CH5424802, AF-802) hydrochloride is a potent, selective ALK inhibitor with IC50 of 1.9 nM.
PC-43320	Alectinib ALK inhibitor	Alectinib (CH5424802, AF-802) is a potent, selective ALK inhibitor with IC50 of 1.9 nM.
PC-42437	NVP-TAE 684 ALK inhibitor	NVP-TAE 684 (TAE684) is a highly potent and selective, orally available ALK inhibitor with IC50 of 3 nM in cell-free assays.
PC-45405	CEP-28122 mesylate ALK inhibitor	CEP-28122 mesylate is a highly potent and selective, orally active ALK inhibitor with IC50 of 1.9 nM.

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