Home Protein Tyrosine Kinase ALK

ALK Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S4967 Ceritinib dihydrochloride Ceritinib (Zykadia, LDK378) dihydrochloride is a selective, orally bioavailable and ATP-competitive inhibitor of ALK with IC50 of 0.2 nM. Ceritinib dihydrochloride also inhibits InsR, IGF-1R and STK22D with IC50 of 7 nM, 8 nM and 23 nM, respectively. Ceritinib exhibits antitomor activity.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
S8583 Repotrectinib (TPX-0005) Repotrectinib (TPX-0005) is a novel ALK/ROS1/TRK inhibitor with the IC50 values of 1.01 nM for WT ALK, 1.26 nM for ALK(G1202R), and 1.08 nM for ALK(L1196M); it is also a potent SRC inhibitor (IC50 5.3 nM).
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Commun Biol, 2024, 7(1):412
Cancer Discov, 2023, 13(3):598-615
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. This compound suppresses cell viability by inducing both cell apoptosis and autophagy.
Sci Rep, 2024, 14(1):8200
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Verified customer review of AZD3463
S2934 Ensartinib dihydrochloride Ensartinib dihydrochloride is a potent new-generation ALK inhibitor with high activity against a broad range of known crizotinib-resistant ALK mutations and CNS metastases. It potently inhibits both wild-type ALK and ALK variants (F1174, C1156Y, L1196M, S1206R, T1151, and G1202R mutants) with in vitro IC50s of <4 nM.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cancer Discov, 2024, OF1-OF20.
Biol Reprod, 2024, ioae090
S7000 AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is a potent and selective ALK inhibitor, as well as an inhibitor of EGFR, and is an analog of AP26113.
Clin Cancer Res, 2015, 21(1):166-74
Clin Cancer Res, 2014, 20(22):5686-96
Jpn J Clin Oncol, 2014, 44(10):963-8
Verified customer review of AP26113-analog (ALK-IN-1)
S8054 ASP3026 ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
iScience, 2024, 27(9):110846
Cell Rep, 2021, 36(7):109515
Invest New Drugs, 2019, 10.1007/s10637-019-00802-7
E1961 NVL-655 (Neladalkib) NVL-655 is a selective inhibitor of anaplastic lymphoma kinase (ALK), with potential antineoplastic activity in the Ba/F3 xenograft model. It also exhibits significant inhibitory activity against ROS1, LTK, PYK2, TRKB, and FAK, with an IC50 ≤10-fold ALK and demonstrates high potency against specific ALK mutations, with an IC50 of <0.73 nM, 7 nM, 3 nM, 3 nM for G1202R, G1202R/L1196M, G1202R/G1269A and G1202R/L1198F respectively.
Pharm Res, 2025, 42(9):1497-1509
S6513 HG-14-10-04 HG-14-10-04 is an inhibitor of ALK.
S6505 X-376 X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer.
E2836 ALK inhibitor 1 ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor which can inhibit testis-specific serine/threonine kinase (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
E1846 TL13-112 TL13-112 is a degrader of anaplastic lymphoma kinase (ALK) with an IC50 of 0.60 nM. It demonstrates anti-proliferative activity in non-small-cell lung cancer (NSCLC) and anaplastic large cell lymphoma (ALCL) cell lines.
E1508 APG-2449 APG-2449 is an orally active inhibitor of ALK/ROS1/FAK. This compound exerts potent and durable antitumor activity in human non-small-cell lung cancer (NSCLC) and ovarian tumor models.
E1865 Envonalkib Envonalkib(TQ-B3139, CT-71, Formula 1) is a potent and orally active inhibitor of ALK, that exhibits IC50 values of 1.96 nM, 35.1 nM, and 61.3 nM for wild-type and mutated L1196M and G1269S-ALK. This compound is also used in the research of non-small cell lung cancer.
E1565 Iruplinalkib Iruplinalkib (WX-0593) is a highly selective oral inhibitor of ALK and ROS1 tyrosine kinase. It exhibits potent and promising antitumor activity in advanced non-small cell lung cancer (NSCLC) with ALK or ROS1 rearrangement.
S0072 MS4078 MS4078 is an inhibitor and PROTAC (degrader) of ALK. This compound reduces the NPM-ALK protein levels in SU-DHL-1 cells and the EML4-ALK protein levels in NCI-H2228 cells with DC50 of 11 nM and 59 nM, respectively. It induces ALK protein degradation via cereblon and proteasome dependent mechanism and potently inhibits proliferation of SU-DHL-1 cells with IC50 of 33 nM.
S8511 Belizatinib (TSR-011) "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "
S9959New Zotizalkib Zotizalkib(TPX-0131) is a compact macrocyclic potent CNS-penetrant, next-generation inhibitor of wild-type ALK and ALK-resistant mutations with an IC50 of 1.4 nM for wild-type ALK. It exhibits antitumor efficacy and can be used in non–small cell lung cancer research.
E1507 Zilurgisertib fumarate Zilurgisertib fumarate(INCB-000928 fumarate, NBU-928 fumarate) is a selective ALK 2 inhibitor.It is under development for the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
E1732 Itacnosertib (TP-0184) Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). This compound reduces hepcidin induction and elevated serum iron levels in turpentine and lung cancer mouse models of ACD.
E0958 ZX-29 ZX-29 is a potent and selective ALK inhibitor with an IC50s of 2.1, 1.3 and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively.
S1068 PF-02341066 (Crizotinib) Crizotinib is a potent inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM in cell-based assays, respectively. It is also a potent ROS1 inhibitor with Ki value less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Signal Transduct Target Ther, 2025, 10(1):124
Cell Rep Med, 2025, S2666-3791(25)00102-8
Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
Verified customer review of PF-02341066 (Crizotinib)
S5190 Crizotinib hydrochloride Crizotinib (PF-02341066) hydrochloride (Xalkori) inhibits tyrosine phosphorylation of c-Met and nucleophosmin (NPM)-anaplastic lymphoma kinase (ALK) with IC50 of of 11 nM and 24 nM in cell-based assays, respectively. Crizotinib hydrochloride is also a potent ROS1 inhibitor with Ki less than 0.025 nM. Crizotinib induces autophagy through inhibition of the STAT3 pathway in multiple lung cancer cell lines.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2829
Cancer Res Commun, 2023, 3(4):659-671
E1783 Conteltinib(CT-707) Conteltinib (CT-707), a potent multikinase inhibitor of ALK, FAK, and Pyk2, shows promising anti-tumor activities. It exhibits significant inhibitory effects on FAK with an IC50 value of 1.6 nM in vitro kinase assay.