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-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-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-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.
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-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	TPX 0005 ALK/ROS1/TRK inhibitor	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	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-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.

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