Anaplastic Lymphoma Kinase (ALK)|Inhibitors Agonists Modulators Antagonists|HmoBio.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
H9566	Iruplinalkib	1854943-32-0	Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement.
H9560	Fidrisertib	2141955-96-4	Fidrisertib(BLU-782) is a activin receptor-like kinase-2 (ALK2) inhibitor with IC50 of <10 nM.
H9557	Envonalkib	1621519-26-3	Envonalkib is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK;Envonalkib can be used for the research of non-small cell lung cancer.
H8950	Itacnosertib	1628870-27-8	Itacnosertib is a potent,an orally ALK2 or ACVR1 protein inhibitor,with IC50 value of 5 nM.
H7639	NVP-TAE 684	761439-42-3	A highly potent and selective, orally available ALK inhibitor with IC50 of 3 nM in cell-free assays; exhibits no significant cross-reactivity against other kinases; blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 2-10 nM, inhibits phosphorylation of NPM-ALK and its downstream effectors and subsequent induction of apoptosis and cell cycle arrest; suppresses lymphomagenesis in in vivo models.
H7638	Lorlatinib	1454846-35-5	A novel CNS-penetrant, ATP-competitive inhibitor of ALK/ROS1 with IC50 of 0.07/0.025 nM respectively; also inhibits ALK L1196M (IC50=0.7 nM) and exhibits selectivity >100-fold for ROS1 over 204 kinases; inhibits crizotinib-resistant mutant ROS1G2032R and ROS1L2026M and orally available in vivo.
H7637	LDN193189 hydrochloride	1062368-62-0	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); efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7; also blocks the transcriptional activity induced by either constitutively active ALK2 R206H or ALK2 Q207D mutant proteins, affects BMP-induced osteoblast differentiation, attenuates ectopic ossification in vivo.
H7636	LDN193189	1062368-24-4	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); efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7; also blocks the transcriptional activity induced by either constitutively active ALK2 R206H or ALK2 Q207D mutant proteins, affects BMP-induced osteoblast differentiation, attenuates ectopic ossification in vivo.
H7635	KRCA-0008	1472795-20-2	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); weakly inhibits IR (IC50=210 nM), inhibits H3122 and BaF3 EML4-ALK L1196M cell proliferation with IC50 of 80 and 68 nM, respectively; demonstrates in vivo efficacy comparable to Crizotinib in xenograft mice model, has drug-like properties without hERG concerns.
H7634	JH-VIII-157-02	1639422-97-1	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); inhibits EML4-ALKWT with IC50 of 2 nM, demonstrates inhibition of CSNK2A1

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