ALK

ALK

ALK, a member of the insulin receptor superfamily and a receptor tyrosine kinase, is primarily expressed in the brain and is thought to play a role in cognition and neuronal development. Adenosine triphosphate (ATP) and a gamma-phosphate group are transferred via ALK to a tyrosine residue on a substrate protein. As a result, it causes the tyrosine residues in its substrate proteins to phosphorylate. Different enzymes (kinases and phosphatases) catalyze the important protein reactions of phosphorylation and dephosphorylation, which are essential to many cellular processes.
ALK gene activation results from fusion with other oncogenes (NPM, EML4, TIM, etc.) or gene amplification, mutation, or protein overexpression and contributes to the development of several human cancers, including anaplastic large cell lymphoma, lung cancer, inflammatory myofibroblastic tumors, and neuroblastoma. ALK is a transmembrane tyrosine kinase receptor that dimerizes and then autophosphorylates the intracellular kinase domain in response to ligand binding to its extracellular domain. Specific inhibitors, like Crizotinib, Ceritinib, Alectinib, etc., have shown to be highly effective in treating ALK-positive non-small cell lung cancer in particular when it becomes activated in cancer.

ALK related products

Structure Cat No. Product Name CAS No. Product Description
V69256 Alectinib-d8 (CH5424802-d8; RO5424802-d8; AF802-d8) 1256585-15-5 Alectinib-d8 is the deuterated form of Alectinib.
V69260 ALK-IN-12 1197958-53-4 ALK-IN-12 is a potent and orally bioactive ALK inhibitor (antagonist) with IC50 of 0.18 nM.
V69264 ALK-IN-13 1197953-88-0 ALK-IN-13 is an ALK inhibitor from patent US20130225528A1, example 19.
V69265 ALK-IN-21 2901889-01-6 ALK-IN-21 (Compound B10) is a potent ALK inhibitor (antagonist) with IC50s of 4.59 nM, 2.07 nM and 5.95 nM for ALKWT, ALKL1196M and ALKG1202R respectively.
V69247 ALK-IN-27 2739866-40-9 ALK-IN-27 (compound 1) is a potent ALK inhibitor.
V69257 ALK-IN-5 2351929-66-1 ALK-IN-5 is a selective, brain barrier-permeable/penetrable (ALK) kinase inhibitor (antagonist) with IC50 of 2.9 nM.
V69258 ALK-IN-9 2359662-39-6 ALK-IN-9 (compound 40) is a potent ALK inhibitor.
V69262 ALK/EGFR-IN-2 2730432-75-2 ALK/EGFR-IN-2 is a potent dual (bifunctional) inhibitor of ALK and EGFR.
V69259 ALK/EGFR-IN-3 2730432-72-9 ALK/EGFR-IN-3 is a dual (bifunctional) inhibitor of ALK and EGFR.
V85845 ALK/ROS1-IN-3
V85477 ALK/ROS1-IN-4 2649878-59-9
V85468 ALK/ROS1-IN-4 hydrate
V69268 ALK2-IN-5 2414149-20-3 ALK2-IN-5 is a pyrazolopyrimidine compound and an ALK2 inhibitor.
V69251 Ascrinvacumab (Anti-ACVRL1 / ALK-1 Reference Antibody (ascrinvacumab); PF-03446962) 1463459-96-2 Ascrinvacumab (PF-03446962) is a human IgG2 monoclonal antibody (mAb) targeting ALK-1.
V86154 CEP-28122 mesylate hydrochloride 1354545-57-5
V69255 CJ-2360 2226742-61-4 CJ-2360 is a potent oral ALK inhibitor (antagonist) with IC50s of 2.2, 4.0, 8.8, 6.3 and 8.9 nM against wild-type ALK and F1197M, G1269A, L1196M and S1206Y ALK mutants, respectively.
V69269 Con B-1 2415537-51-6 ConB-1 is a selective ALK inhibitor (antagonist) with low toxicity to normal cells.
V69252 CPD-1224 2891620-68-9 CPD-1224 is an orally bioavailable ALK inhibitor and an ALK inhibitor analogue coupled to cereblon ligand.
V69253 Envonalkib 1621519-26-3 This product is discontinued due to commercial reason. Envonalkib is a potent and orally bioactive ALK inhibitor (antagonist) with IC50s of 1.96 nM, 35.1 nM and 61.3 nM against WT and mutant L1196M and G1269S-ALK, respectively.
V69254 Ficonalkib 2233574-95-1 Ficonalkib is a potent inhibitor of anaplastic lymphoma kinase (ALK), a tyrosine kinase receptor.
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