Signaling Pathway

ALK

ALK

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ALK (Anaplastic lymphoma kinase) is an enzyme that in humans is encoded by the ALK gene. ALK is a membrane associated tyrosine kinase receptor of the insulin receptor superfamily. The function of the full-length ALK receptor is poorly understood. It has a probable role in the central and peripheral nervous system development and maintenance. ALK is a dependence receptor, which may exert antagonist functions, proapoptotic or antiapoptotic, depending on the absence or presence of a ligand. Dependence receptors have a potential role in cancer and development. Ligands available for this demonstration were agonist anti-ALK antibodies. ALK is still an orphan receptor, given the high level of controversy about pleiotrophin and midkine, which have been proposed as ligands by Stoica et al.

ALK Inhibitors & Modulators (31)

Product Name Catalog No. Brief Description
ALK inhibitor 1

HY-15357

ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.

ALK inhibitor 2

HY-15358

ALK inhibitor 2 is a novel and selective inhibitor for the ALK kinase.

ALK-IN-1

HY-13464

ALK-IN-1 is a potent and selective active inhibitor of anaplastic lymphoma kinase(ALK), Patent US20140066406 A1.

ASP3026

HY-13326

ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.

AZD-3463

HY-15609

AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.

Brigatinib

HY-12857

Brigatinib is a highly potent and selective investigational ALK inhibitor with mean IC50 value < 100 nM in Ba/F3 cells.

CEP-28122

HY-18030

CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.

CEP-28122 mesylate salt

HY-18030A

CEP-28122 mesylate salt is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.

CEP-37440

HY-15841

CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).

CH5424802

HY-13011

CH5424802(AF 802; Alectinib) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.

CH5424802 Hydrochloride

HY-13011A

CH5424802 Hcl (AF 802 Hcl; Alectinib Hcl) is a potent ALK inhibitor with IC50 of 1.9 nM, sensitive to L1196M mutation.

Crizotinib

HY-50878

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.

Crizotinib hydrochloride

HY-50878A

Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK.

DMH-1

HY-12273

DMH-1 is a potent and selective BMP inhibitor with IC50s of 27/107.9/<5 nM for ALK1/2/3 respectively; inactive on ALK5, BMPR2, AMPK and VEGFR2.

Ensartinib

HY-16590

Ensartinib is a potent inhibitor of ALK, which is used to treat non-small-cell lung cancer.

Entrectinib

HY-12678

Entrectinib (RXDX-101) is an oral pan-Trk, ROS1, and ALK inhibitor, with IC50 of 1.7/0.1/0.1 nM, 0.2 nM, and 1.6 nM for Trk A/B/C, ROS1, and ALK, respectively.

GSK1838705A

HY-13020

GSK1838705A is a potent small-molecule IGF-1R, the insulin receptor and anaplastic lymphoma kinase (ALK) inhibitor with IC50 of 2.0, 1.6 and 0.5 nM, respectively.

HG-14-10-04

HY-15801

HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM.

K02288

HY-12278

K02288 is a novel small molecule inhibitor of ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; specific for ALK1,2,3,6 over ALK4,5; inhibitor of BMP signaling.

KRCA-0008

HY-12331

KRCA-0008 is a potent and selective ALK/Ack1 inhibitor with IC50 of 12 nM/4 nM for ALK and Ack1 respectively; displays drug-like properties without hERG liability.