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Catalog No. Product Name Information Product Use Citations Product Validations
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
Cancers (Basel), 2022, 14(6)1378
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
Cancers (Basel), 2022, 14(6)1378
Mol Cancer Res, 2022, molcanres.MCR-22-0025-E.2022
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
J Clin Invest, 2021, 131(11)146987
Mol Cancer Ther, 2021, molcanther.0344.2021
Front Oncol, 2020, 12;10:700
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
Nature, 2021, 600(7888):319-323
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
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
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
S8696 2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
Nat Commun, 2021, 12(1):4794
Cancers (Basel), 2021, 13(14)3475
Cancer Sci, 2021, 112(10):4075-4086
S8901 Taletrectinib (DS-6051b) Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
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
Cancers (Basel), 2022, 14(6)1378
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
Cancers (Basel), 2022, 14(6)1378
Mol Cancer Res, 2022, molcanres.MCR-22-0025-E.2022
S7014 Merestinib (LY2801653) Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively.
J Clin Invest, 2021, 131(11)146987
Mol Cancer Ther, 2021, molcanther.0344.2021
Front Oncol, 2020, 12;10:700
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
Nature, 2021, 600(7888):319-323
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
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
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
S8696 2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.
Nat Commun, 2021, 12(1):4794
Cancers (Basel), 2021, 13(14)3475
Cancer Sci, 2021, 112(10):4075-4086
S8901 Taletrectinib (DS-6051b) Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109