Anaplastic lymphoma kinase (ALK) Inhibitor

WY-135 is an ALK (IC₅₀=1.4 nM) and ROS1 (IC₅₀=1.1 nM) dual inhibitor.

Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK^L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC₅₀s of 15-43 nM (ALK^L1196), 14-80 nM (ALK^G1269A), 38-50 nM (ALK^1151Tins), 77-113 nM (ALK^G1202R), respectively.

CEP-14513 is an ALK inhibitor with an IC₅₀ of 4 nM. CEP-14513 also inhibits insulin receptor, VEGFR2, TIE2 and DLK kinases, but does not inhibit MET, IKKβ, or CDK1/2/5. CEP-14513 induces cancer cell apoptosis. CEP-14513 is applicable to research related to non-small cell lung cancer, anaplastic large cell lymphoma, inflammatory myofibroblastic tumor, and diffuse large B-cell lymphoma.

CJ-2360 is a potent and orally active ALK inhibitor 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. CJ-2360 displays potent inhibitory activity against two clinically reported ALK mutants (C1156Y and L1196M) and a few other kinases (LTK, MERTK, CLK1, DAPK1, and DAPK2) among the 468 kinases evaluated.

Crizotinib-amide-PEG2-NH2 is a MET ligand (HY-50878) linker conjugate. Crizotinib-amide-PEG2-NH2 can be used for synthesis of MET degrader OZD-MET 01 (HY-177893).

ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC₅₀ of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research.

Brigatinib-¹³C₆ is the ¹³C-labeled Brigatinib. Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor, with an IC₅₀ of 0.6 nM.

ALK protein ligand-1 (Compound A1), a ligand for the anaplastic lymphoma kinase (ALK) protein, is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs) that exhibits inhibitory effects on ALK. ALK protein ligand-1 can be used in the synthesis of AP-1 (HY-169481).

ALK-IN-37 is an orally active type I₁/₂ allosteric inhibitor of anaplastic lymphoma kinase (ALK) with an IC₅₀ of 9.58 nM. ALK-IN-37 induces cell apoptosis, inhibits colony formation, suppresses cell migration, and exerts antiproliferative effects in cancer cells overexpressing ALK. ALK-IN-37 can be used in research related to non-small cell lung cancer.

ALK5-IN-87 is a potent lung-restricted ALK5 inhibitor with a pK_i of 10.13. ALK5-IN-87 exerts antifibrotic activity in a mouse model of lung fibrosis. ALK5-IN-87 can be used for the research of idiopathic pulmonary fibrosis.

ALK/EGFR-IN-3 is a dual inhibitor of ALK and EGFR. ALK/EGFR-IN-3 inhibits the cell proliferation of H1975, PC9, and Baf3-EML4-ALK cancer cell lines with IC₅₀s of 0.1360, 0.0332, and 0.0339 μM, respectively.

Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC₅₀s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition.

ALK-IN-29 (compound 4c) has a certain inhibitory effect on tyrosine protein kinases ALK, CDK2/CyclinE1 and FAK, among which the strongest inhibitory effect on ALK kinase is 40.63% at a concentration of 10 μM. ALK-IN-29 can be used for anti-cancer research.

ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

TRK/ALK-IN-1 (compound 21) is a potent and dual inhibitor of TRK and ALK. TRK/ALK-IN-1 in the enzymatic assays is in good accordance with anti-proliferative activity with IC₅₀ values of 2.2, 9.3 and 38 nM towards TRKA, ALK^WT and ALK^L1196M, respectively. TRK/ALK-IN-1 has the potential for the research of cancer diseases.

PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC₅₀ of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research.

M4K2163 is a ALK2 inhibitor that serves as a target protein ligand for the synthesis of PROTACs, such as M4K3250 (HY-183718). M4K2163 induces cytotoxic effects in glioblastoma cells. M4K2163 can be used in the research of diffuse intrinsic pontine glioma and glioblastoma.

ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor. ALK2-IN-5 can inhibit ALK2 activity and FGFR activity. ALK2-IN-5 can be used for the research of disorders associated with ALK2 activity and/or FGFR activity, such as cancer.

ALK-IN-24 is an orally active ALK inhibitor with an IC₅₀ value of 1.7 nM. ALK-IN-24 also inhibits insulin receptor kinase with an IC₅₀ value of 6 nM. ALK-IN-24 suppresses the proliferation of lung adenocarcinoma cells. ALK-IN-24 inhibits ALK-driven tumor growth in xenograft mouse models. ALK-IN-24 can be used in research related to non-small cell lung cancer.

CM-118 is a potent and selective c-Met and ALK inhibitor. CM-118 inhibits the HGF-induced c-Met phosphorylation. CM-118 inhibits phosphorylation of ALK, EML4-ALKv1, ALK F1174L, and EMl4-ALKv1 L1196M, with respective IC₅₀ values 0.92, 1.25, 1.9, and 3.5 μM. CM-118 exhibits anticancer activity against cancers dependent on the c-Met or ALK oncogenic pathways.