ROS1

ROS1 Products

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  • ROS1 Inhibitors (9)
  • New ROS1 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
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
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
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
Cancer Commun (Lond), 2020, 11
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.
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
E1409New Zidesamtinib Zidesamtinib (NVL-520) is a potent brain-penetrating inhibitor of ROS1 tyrosine kinase with IC50 of 0.7 nM for wild-type ROS1 . It acts as a potential antineoplastic agent and can be used for the research of cancer.
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
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
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
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
Cancer Commun (Lond), 2020, 11
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.
Transl Lung Cancer Res, 2022, 11(11:2216-2229)
Mol Cancer Ther, 2021, molcanther.0965.2020
Mol Cancer Ther, 2021, 20(9):1653-1662
E1409New Zidesamtinib Zidesamtinib (NVL-520) is a potent brain-penetrating inhibitor of ROS1 tyrosine kinase with IC50 of 0.7 nM for wild-type ROS1 . It acts as a potential antineoplastic agent and can be used for the research of cancer.
E1409New Zidesamtinib Zidesamtinib (NVL-520) is a potent brain-penetrating inhibitor of ROS1 tyrosine kinase with IC50 of 0.7 nM for wild-type ROS1 . It acts as a potential antineoplastic agent and can be used for the research of cancer.

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Tags: ROS1 inhibitor|ROS1 agonist|ROS1 activator|ROS1 inducer|ROS1 antagonist|ROS1 signaling pathway|ROS1 assay kit