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Catalog No. Product Name Information Product Use Citations Product Validations
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.
S1068 Crizotinib (PF-02341066) Crizotinib (PF-02341066) 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Dis, 2022, 13(4):351
S1108 TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
EBioMedicine, 2022, 78:103963
Cancers (Basel), 2022, 14(6)1517
Thorac Cancer, 2022, 10.1111/1759-7714.14372
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.
Cancer Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
Cell, 2019, 36(2):179-193
S2762 Alectinib (CH5424802) Alectinib (CH5424802, AF-802, RG-7853) 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.
NPJ Precis Oncol, 2022, 6(1):5
Sci Rep, 2022, 12(1):6345
Thorac Cancer, 2022, 10.1111/1759-7714.14372
S2934 Ensartinib (X-396) dihydrochloride Ensartinib (X-396) 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.
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
CU Digital Repository, 2020, N/A
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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Nature, 2021, 600(7888):319-323
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.
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Dis, 2022, 13(4):351
Cancers (Basel), 2022, 14(6)1378
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.
NPJ Precis Oncol, 2022, 6(1):5
Thorac Cancer, 2022, 10.1111/1759-7714.14372
Nature, 2021, 600(7888):319-323
S6505 X-376 X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer.
S6513 HG-14-10-04 HG-14-10-04 is an inhibitor of ALK.
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
Jpn J Clin Oncol, 2014, 44(10):963-8
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Sci Rep, 2022, 12(1):6345
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.
Cancers (Basel), 2020, 12(9)E2668
Aging (Albany NY), 2020, 7;12(9):8221-8240
Burns Trauma, 2020, 8:tkaa025
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.
NPJ Precis Oncol, 2022, 6(1):11
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Discov, 2022, 8(1):221
S7998 Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) 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 Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nature, 2021, 600(7888):319-323
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
S8229 Brigatinib (AP26113) Brigatinib (AP26113) 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.
NPJ Precis Oncol, 2022, 6(1):11
NPJ Precis Oncol, 2022, 6(1):5
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
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). "
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 Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
A5397 ACVRL1 Rabbit Recombinant mAb ACVRL1 Rabbit Recombinant mAb detects endogenous level of total ACVRL1.
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.
S1068 Crizotinib (PF-02341066) Crizotinib (PF-02341066) 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.
Cancer Cell, 2022, S1535-6108(21)00662-0
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Dis, 2022, 13(4):351
S1108 TAE684 (NVP-TAE684) TAE684 (NVP-TAE684) is a potent and selective ALK inhibitor with IC50 of 3 nM in a cell-free assay, 100-fold more sensitive for ALK than InsR. TAE684 (NVP-TAE684) induces cell cycle arrest and apoptosis.
EBioMedicine, 2022, 78:103963
Cancers (Basel), 2022, 14(6)1517
Thorac Cancer, 2022, 10.1111/1759-7714.14372
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.
Cancer Cell, 2021, S1535-6108(21)00383-4
J Invest Dermatol, 2020, 3 pii: S0022-202X(20)31407-X
Cell, 2019, 36(2):179-193
S2762 Alectinib (CH5424802) Alectinib (CH5424802, AF-802, RG-7853) 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.
NPJ Precis Oncol, 2022, 6(1):5
Sci Rep, 2022, 12(1):6345
Thorac Cancer, 2022, 10.1111/1759-7714.14372
S2934 Ensartinib (X-396) dihydrochloride Ensartinib (X-396) 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.
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
CU Digital Repository, 2020, N/A
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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Nature, 2021, 600(7888):319-323
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.
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Dis, 2022, 13(4):351
Cancers (Basel), 2022, 14(6)1378
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.
NPJ Precis Oncol, 2022, 6(1):5
Thorac Cancer, 2022, 10.1111/1759-7714.14372
Nature, 2021, 600(7888):319-323
S6505 X-376 X-376 is an ALK inhibitor and potentially useful in non-small cell lung cancer.
S6513 HG-14-10-04 HG-14-10-04 is an inhibitor of ALK.
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
Jpn J Clin Oncol, 2014, 44(10):963-8
S7083 Ceritinib (LDK378) Ceritinib (LDK378) is 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.
Cancer Res, 2022, 82(2):307-319
NPJ Precis Oncol, 2022, 6(1):11
Sci Rep, 2022, 12(1):6345
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.
Cancers (Basel), 2020, 12(9)E2668
Aging (Albany NY), 2020, 7;12(9):8221-8240
Burns Trauma, 2020, 8:tkaa025
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.
NPJ Precis Oncol, 2022, 6(1):11
NPJ Precis Oncol, 2022, 6(1):5
Cell Death Discov, 2022, 8(1):221
S7998 Entrectinib (RXDX-101) Entrectinib (RXDX-101, NMS-E628) 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 Res, 2022, canres.1397.2021
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Nature, 2021, 600(7888):319-323
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
S8229 Brigatinib (AP26113) Brigatinib (AP26113) 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.
NPJ Precis Oncol, 2022, 6(1):11
NPJ Precis Oncol, 2022, 6(1):5
Mol Pharmacol, 2022, MOLPHARM-AR-2021-000287
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). "
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 Res, 2022, canres.1397.2021
Nature, 2021, 600(7888):319-323
Clin Cancer Res, 2020, clincanres.2585.2020
A5397 ACVRL1 Rabbit Recombinant mAb ACVRL1 Rabbit Recombinant mAb detects endogenous level of total ACVRL1.
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