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
|
|