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  • ALK Inhibitors (24)
  • New ALK Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1068 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.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S7083 Ceritinib 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.
Nat Commun, 2024, 15(1):51
iScience, 2024, 27(2):109015.
Clin Cancer Res, 2023, 29(7):1317-1331
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. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
EMBO Rep, 2023, 24(7):e56937
J Biol Chem, 2023, 299(6):104825
Pharmacol Res Perspect, 2023, 11(1):e01047
S2762 Alectinib 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.
Nat Commun, 2024, 15(1):51
Clin Cancer Res, 2023, 29(7):1317-1331
Clin Cancer Res, 2023, 29(5):943-956
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
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
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.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2601
Clin Cancer Res, 2023, 29(7):1317-1331
S7998 Entrectinib 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.
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Biomolecules, 2023, 13(3)438
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.
J Thorac Oncol, 2023, S1556-0864(23)00797-9
NPJ Precis Oncol, 2023, 7(1):12
J Med Chem, 2023, 66(17):12130-12140
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.
Biomolecules, 2023, 13(3)438
Exp Mol Med, 2022, 54(8):1225-1235
NPJ Precis Oncol, 2022, 6(1):5
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
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.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Cancer Res, 2022, canres.1397.2021
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S7000 AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
Clin Cancer Res, 2015, 21(1):166-74
Clin Cancer Res, 2014, 20(22):5686-96
Clin Cancer Res, 2014, 20(22):5686-96
S8054 ASP3026 ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
Cell Rep, 2021, 36(7):109515
Invest New Drugs, 2019, 10.1007/s10637-019-00802-7
Mol Cancer Ther, 2018, 17(1):222-231
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.
Biomed Pharmacother, 2022, 158:114162
Cancers (Basel), 2022, 14(9)2341
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
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).
S0072 MS4078 MS4078 is an inhibitor and PROTAC (degrader) of ALK. MS4078 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. MS4078 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). "
E1507New 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.
E1732New Itacnosertib (TP-0184) Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). Itacnosertib 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 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.
Nat Commun, 2024, 15(1):1009
Nat Commun, 2024, 15(1):51
Cancer Discov, 2023, 13(3):598-615
S7083 Ceritinib 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.
Nat Commun, 2024, 15(1):51
iScience, 2024, 27(2):109015.
Clin Cancer Res, 2023, 29(7):1317-1331
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. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
EMBO Rep, 2023, 24(7):e56937
J Biol Chem, 2023, 299(6):104825
Pharmacol Res Perspect, 2023, 11(1):e01047
S2762 Alectinib 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.
Nat Commun, 2024, 15(1):51
Clin Cancer Res, 2023, 29(7):1317-1331
Clin Cancer Res, 2023, 29(5):943-956
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
Cancer Res Commun, 2023, 3(4):659-671
J Exp Clin Cancer Res, 2022, 41(1):309
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.
Cancer Discov, 2023, 13(3):598-615
Nat Commun, 2023, 14(1):2601
Clin Cancer Res, 2023, 29(7):1317-1331
S7998 Entrectinib 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.
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Biomolecules, 2023, 13(3)438
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.
J Thorac Oncol, 2023, S1556-0864(23)00797-9
NPJ Precis Oncol, 2023, 7(1):12
J Med Chem, 2023, 66(17):12130-12140
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.
Biomolecules, 2023, 13(3)438
Exp Mol Med, 2022, 54(8):1225-1235
NPJ Precis Oncol, 2022, 6(1):5
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
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.
Exp Mol Med, 2022, 54(8):1225-1235
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
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); also a potent SRC inhibitor (IC50 5.3 nM).
Cancer Discov, 2023, 13(3):598-615
EMBO Mol Med, 2023, 10.15252/emmm.202217367
Cancer Res, 2022, canres.1397.2021
S7106 AZD3463 AZD3463 is a novel orally bioavailable ALK inhibitor with Ki of 0.75 nM, which also inhibits IGF1R with equivalent potency. AZD3463 suppresses cell viability by inducing both cell apoptosis and autophagy.
bioRxiv, 2023, 10.1101/2023.12.19.572304
Burns Trauma, 2020, 8:tkaa025
Cancers (Basel), 2020, 12(9)E2668
S7000 AP26113-analog (ALK-IN-1) AP26113-analog (ALK-IN-1) is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR.
Clin Cancer Res, 2015, 21(1):166-74
Clin Cancer Res, 2014, 20(22):5686-96
Clin Cancer Res, 2014, 20(22):5686-96
S8054 ASP3026 ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM. Phase 1.
Cell Rep, 2021, 36(7):109515
Invest New Drugs, 2019, 10.1007/s10637-019-00802-7
Mol Cancer Ther, 2018, 17(1):222-231
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.
Biomed Pharmacother, 2022, 158:114162
Cancers (Basel), 2022, 14(9)2341
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
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).
S0072 MS4078 MS4078 is an inhibitor and PROTAC (degrader) of ALK. MS4078 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. MS4078 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). "
E1507New 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.
E1732New Itacnosertib (TP-0184) Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). Itacnosertib 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.
E1507New 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.
E1732New Itacnosertib (TP-0184) Itacnosertib (TP-0184) is a small-molecule inhibitor of the BMP type 1 receptor ALK2 (also known as ACVR1). Itacnosertib reduces hepcidin induction and elevated serum iron levels in turpentine and lung cancer mouse models of ACD.

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