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ALK inhibitors

ALK (anaplastic lymphoma kinase), is an orphan receptor discovered in anaplastic large cell lymphomas (ALCL) plays a key role in the normal development and function of the nervous system. ALK directly binds to insulin receptor substrate 1 (IRS1), SRC homology 2 domain-containing (SHC) and SRC start to activate MAPK signaling pathway by activating the Ras–extracellular signalregulated kinase (ERK) pathway. Phospholipase C-γ (PLCγ) which is directly bound and activated by ALK result in activation protein kinase C (PKC) by mobilizing calcium stores from the endoplasmic reticulum. ALK can also induce mammalian target of rapamycin (mTOR) activation which  is transduced through the ERK signalling pathway and ends in the phosphorylation of the mTOR targets ribosomal protein S6 kinase (p70S6K) and S6 ribosomal protein (S6RP).

Other Protein Tyrosine Kinase Related Inhibitors

VEGFR EGFR c-Met PDGFR CSF-1R IGF-1R c-Kit Tie-2 HER2 c-RET
Cat.No. Product Name Information Product Use Citations Product Validations
S2762 Alectinib (CH5424802) Alectinib is a potent ALK inhibitor with IC50 of 1.9 nM in cell-free assays, sensitive to L1196M mutation and higher selectivity for ALK than PF-02341066, NVP-TAE684 and PHA-E429.
Signal Transduct Target Ther, 2025, 10(1):124
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Death Dis, 2025, 16(1):194
Verified customer review of Alectinib (CH5424802)
S7530 Vactosertib (TEW-7197) Vactosertib  (TEW-7197, EW-7197) is a highly potent, selective, and orally bioavailable TGF-β receptor ALK4/ALK5 inhibitor with IC50 of 13 nM and 11 nM, respectively. Phase 1.
Mol Ther, 2025, 33(12):6130-6145
Nat Commun, 2024, 15(1):7388
Cells, 2024, 13(10)879
Verified customer review of Vactosertib (TEW-7197)
S2230 Galunisertib (LY2157299) Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI / ALK5) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
Signal Transduct Target Ther, 2025, 10(1):332
Signal Transduct Target Ther, 2025, 10(1):257
Exp Mol Med, 2025, 57(6):1324-1338
Verified customer review of Galunisertib (LY2157299)
S7998 Entrectinib (Rxdx-101) Entrectinib is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Entrectinib (RXDX-101) induces autophagy. Phase 2.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cancer Gene Ther, 2025, 10.1038/s41417-025-00874-z
Mol Cancer Ther, 2025, 10.1158/1535-7163.MCT-25-0025
Verified customer review of Entrectinib (Rxdx-101)
S7083 Ceritinib (LDK378) Ceritinib is a potent inhibitor against ALK with IC50 of 0.2 nM in cell-free assays. Ceritinib (LDK378) also inhibits IGF-1R, InsR, STK22D and FLT3 with IC50 of 8 nM, 7 nM, 23 nM and 60 nM, respectively. Phase 3.
Signal Transduct Target Ther, 2025, 10(1):124
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Mol Life Sci, 2025, 82(1):314
Verified customer review of Ceritinib (LDK378)
S1108 TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor which blocked the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM, 100-fold more sensitive for ALK than InsR. This compound induces cell cycle arrest and apoptosis.
Adv Sci (Weinh), 2025, 12(17):e2416802
Sci Rep, 2024, 14(1):8200
EMBO Rep, 2023, 24(7):e56937
Verified customer review of TAE684 (NVP-TAE684)
S7536 Lorlatinib (PF-6463922) Lorlatinib (PF-6463922) is a potent, dual ALK/ROS1 inhibitor with Ki of <0.02 nM, <0.07 nM, and 0.7 nM for ROS1, ALK (WT), and ALK (L1196M), respectively. PF-06463922 induces apoptosis. Phase 1.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Death Dis, 2025, 16(1):194
Mol Oncol, 2025, 19(2):519-539
Verified customer review of Lorlatinib (PF-6463922)
S8229 Brigatinib Brigatinib is a potent and selective ALK (IC50, 0.6 nM) and ROS1 (IC50, 0.9 nM) inhibitor. It also inhibits IGF-1R, FLT3, and mutant variants of FLT3 (D835Y) and EGFR with lower potentcy.
Leukemia, 2025, 10.1038/s41375-025-02682-8
Cell Death Dis, 2025, 16(1):194
Toxicol Appl Pharmacol, 2025, 498:117310
Verified customer review of Brigatinib
S5232 Alectinib (CH5424802) hydrochloride Alectinib (AF802, CH5424802, RO5424802, RG-7853) is a second generation oral drug that selectively inhibits the activity of anaplastic lymphoma kinase (ALK) tyrosine kinase.
iScience, 2024, 27(9):110846
Biomolecules, 2023, 13(3)438
Exp Mol Med, 2022, 54(8):1225-1235
S2703 GSK1838705A GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
Sci Signal, 2022, 15(747):eabj5879
Cancer Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
Verified customer review of GSK1838705A

Signaling Pathway Map