alk

Neladalkib (NVL-655) is a selective and brain-permeable ALK inhibitor with antitumor activity that inhibits a variety of ALK-mutant oncoproteins, and may be useful in the study of non-small cell cancers.

A 83-01 (ALK5 Inhibitor IV) is an inhibitor of the TGF-β type I receptors ALK5, ALK4, and ALK7 (IC50=12 45 7.5 nM). A 83-01 promotes the reprogramming of mouse fibroblasts into iPSCs. A 83-01 can be used in organoid cultures.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

Entrectinib (RXDX-101) is a Trk, ROS1, and ALK inhibitor that inhibits TrkA, TrkB, TrkC, ROS1, and ALK (IC50=1 3 5 12 7 nM) with oral activity and blood-brain-barrier penetration. Entrectinib exhibits both antitumor and CNS activity.

CEP-28122 is a highly potent and selective, orally active ALK inhibitor.

HG-14-10-04 is a potent and specific ALK (anaplastic lymphoma kinase) inhibitor.

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met, with IC50 values of 20 nM and 8 nM, respectively.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

ALK-IN-1 is a Brigatinib analog and an ALK inhibitor commonly used in anti-tumor research.

ALK-IN-5 is a potent, selective, and brain-penetrant inhibitor of anaplastic lymphoma kinase (ALK) with an IC50 of 2.9 nM.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

ALK-IN-26 is an ALK inhibitor with potential anticancer activity, demonstrating antiproliferative effects against glioblastoma and inducing apoptosis, autophagy, and necrosis.

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 trimesylate salt inhibits IGF1R activity and can be used in the study of non-small cell lung cancer.

ALK-IN-6 is an orally bioavailable inhibitor of anaplastic lymphoma kinase (ALK, IC50s: 71 nM, 18.72 nM, and 36.81 nM for ALK wild, ALK F1196M and ALK F1174L).

ALK ROS1 inhibitor 2e HCL possesses anti-apoptotic, anti-proliferative and anti-tumour activities.

ALK ROS1-IN-1 is a potent and selective anti-crizotinib-resistant ALK ROS1 dual inhibitor (IC50s: 0.530 μM and 0.174 μM for ROS1 and ALK enzyme).

PROTAC ALK degrader-3 (4B) is an orally active PROTAC-based ALK degrader, efficiently inducing sustained degradation of ALK fusion protein and significant inhibition of downstream pathways in Karpas 299 cells with an IC50 of 119.33 nM. This compound exhibits antitumor activity.

ALK-IN-29 (compound 4c) exhibits inhibitory effects on tyrosine protein kinases such as ALK, CDK2 CyclinE1, and FAK, with the strongest inhibition observed against ALK kinase, displaying a 40.63% inhibition rate at a concentration of 10 μM. ALK-IN-29 is applicable in cancer research.

ALK ROS1-IN-5 (compound X4) is a selective inhibitor of ALK and ROS1 kinases, with IC50 values of 0.512 μM for ALK and 0.766 μM for ROS1. It inhibits H2228 cells with an IC50 of 0.034 μM and induces apoptosis in cancer cells in a dose-dependent manner. Additionally, ALK ROS1-IN-5 effectively suppresses the expression of p-ALK and p-ERK in cancer cells.

ALK protein ligand-1 (Compound A1) is an ALK protein ligand, acting as a ligand for the target protein in PROTACs, demonstrating inhibitory effects on ALK. It is also useful in the synthesis of AP-1.

ALK/PI3K/AKT-IN-1 (Compound 45) effectively inhibits the proliferation of cancer cell lines A549, H1975, and PC9, with IC50 values of 0.44, 0.83, and 1.51 μM, respectively. This compound enhances the expression of p21 and p27, and decreases the activity of CDK2 and p-Rb, causing cell cycle arrest at the G1 phase. It suppresses the ALK/PI3K/AKT signaling pathway, promotes mitochondrial membrane potential depolarization, and induces apoptosis in A549 cells. Furthermore, ALK/PI3K/AKT-IN-1 inhibits the formation and growth of A549 cell spheres.

ALK-001 is a vitamin A analog, which may be used to treat Stargardt disease.