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ROS1 inhibitor

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-131003
    Taletrectinib
    1 Publications Verification

    DS-6051b; AB-106; IBI-344

    ROS Kinase Cancer
    Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
    Taletrectinib
  • HY-152292

    NVL-520; NUV-520

    ROS Kinase Cancer
    Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer .
    Zidesamtinib
  • HY-145574

    WX-0593

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and ROS1 tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement .
    Iruplinalkib
  • HY-157391

    ROS Kinase Anaplastic lymphoma kinase (ALK) Cancer
    ALK/ROS1-IN-3 (compound C01) is a ROS1 and ALK dual inhibitor with IC50s of 42.3 nM and 49.1 nM for ROS1 G2032R and ALK G1202R, respectively .
    ALK/ROS1-IN-3
  • HY-161975

    ROS Kinase Cancer
    ROS1-IN-2 (Compound 3) is a ROS1 inhibitor. ROS1-IN-2 can be used in the study of cancer .
    ROS1-IN-2
  • HY-150974

    ROS Kinase Cancer
    ROS1-IN-1 (Compound 31) is a potent and selective ROS1 kinase inhibitor with an IC50 of 0.097 μM .
    ROS1-IN-1
  • HY-160172

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    ALK/ROS1-IN-4 (example 13) is a dual inhibitor of ALK and ROS1 kinase .
    ALK/ROS1-IN-4
  • HY-160172A

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    ALK/ROS1-IN-4 (hydrate) (example 13) is a dual inhibitor of ALK and ROS1 kinase .
    ALK/ROS1-IN-4 hydrate
  • HY-130794

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant ALK/ROS1 dual inhibitor, with IC50s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.
    ALK/ROS1-IN-1
  • HY-131003A

    DS-6051b free base; AB-106 free base; IBI-344 free base

    ROS Kinase Cancer
    Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .
    Taletrectinib free base
  • HY-159147

    PROTACs ROS Kinase Apoptosis Cancer
    SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
    SIA​​IS039
  • HY-112801

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK WT, ROS1 WT, ALK L1196M and ALK G1202R, respectively .
    F-1
  • HY-111416

    Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer
    WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
    WY-135
  • HY-153743

    ROS Kinase Trk Receptor Cancer
    Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and ROS1 (IC50=3.0 nM and 104 nM respectively) .
    Protein kinase inhibitor 4
  • HY-12215
    Lorlatinib
    25+ Cited Publications

    PF-06463922

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib
  • HY-135509

    PF-06463922 acetate

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib acetate has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib acetate
  • HY-155163

    Anaplastic lymphoma kinase (ALK) ROS Kinase FAK Others Cancer
    APG-2449 is an orally active ALK/ROS1/FAK inhibitor. APG-2449 shows antitumor activity in mouse models of non-small cell lung cancer (NSCLC) .
    APG-2449
  • HY-12215R

    Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis Cancer
    Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively .
    Lorlatinib (Standard)
  • HY-103022
    Repotrectinib
    3 Publications Verification

    TPX-0005

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Cancer
    Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity .
    Repotrectinib
  • HY-12678
    Entrectinib
    20+ Cited Publications

    NMS-E628; RXDX-101

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib
  • HY-50878
    Crizotinib
    Maximum Cited Publications
    65 Publications Verification

    PF-02341066

    Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib
  • HY-50878B

    PF-02341066 acetate

    Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR Cancer
    Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib acetate inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition .
    Crizotinib acetate
  • HY-B0847S

    Fungal Reactive Oxygen Species Infection
    Propiconazole-d7 is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].
    Propiconazole-d7
  • HY-50878S

    PF-02341066-d5

    Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib-d5 is the deuterium labeled Crizotinib. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib-d5
  • HY-12678R

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib (Standard)
  • HY-50878A
    Crizotinib hydrochloride
    Maximum Cited Publications
    65 Publications Verification

    PF-02341066 hydrochloride

    Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib hydrochloride
  • HY-50878R

    Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib (Standard) is the analytical standard of Crizotinib. This product is intended for research and analytical applications. Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition .
    Crizotinib (Standard)
  • HY-120387

    ROS Kinase Anaplastic lymphoma kinase (ALK) TAM Receptor c-Met/HGFR Cancer
    SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models .
    SMU-B
  • HY-12678S

    NMS-E628-d4; RXDX-101-d4

    ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Isotope-Labeled Compounds Cancer
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib-d4
  • HY-50878AS

    PF-02341066-d9 hydrochloride

    c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds Cancer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib-d9 hydrochloride
  • HY-15514A
    Merestinib dihydrochloride
    5 Publications Verification

    LY2801653 dihydrochloride

    c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor Cancer
    Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
    Merestinib dihydrochloride
  • HY-15514
    Merestinib
    5 Publications Verification

    LY2801653

    c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor Cancer
    Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
    Merestinib
  • HY-12678S1

    NMS-E628-d8; RXDX-101-d8

    Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase Cancer
    Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC50 values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice .
    Entrectinib-d8
  • HY-155178

    EGFR Cancer
    Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC50 of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC50 of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC50 values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC50 values < 10 nM) under hypoxic condition .
    Antiproliferative agent-34
  • HY-156360

    Xanthine Oxidase Reactive Oxygen Species Inflammation/Immunology
    Xanthine oxidase-IN-12 (Compound 11) is a xanthine oxidase (XO) inhibitor with an IC50 of 91 nM. Xanthine oxidase-IN-12 also has antioxidant activity and reduces intracellular ROS .
    Xanthine oxidase-IN-12
  • HY-144697

    p38 MAPK Apoptosis Reactive Oxygen Species Cancer
    p38 MAPK-IN-3 (Compound 2c) is a p38α MAPK inhibitor. p38 MAPK-IN-3 has antitumor activities and induces apoptosis and ROS .
    p38 MAPK-IN-3
  • HY-147795

    NAMPT Apoptosis Reactive Oxygen Species Cancer
    Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC50 of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and ROS .
    Nampt-IN-8
  • HY-N11887

    Reactive Oxygen Species Inflammation/Immunology
    Linocinnamarin is a nature product that could be isolated from Fragaria ananassa Duch. Linocinnamarin has anti-inflammatory activity. Linocinnamarin inhibits antigen-stimulated elevation of intracellular free Ca 2+ concentration and reactive oxygen species (ROS) .
    Linocinnamarin
  • HY-163862

    PPAR Reactive Oxygen Species Inflammation/Immunology
    PPARα agonist 3 (Compound A229) is a PPARα agonist (EC50: 590 nM). PPARα agonist 3 inhibits TBHP or 4-HNE (HY-113466)-induced production of ROS .
    PPARα agonist 3
  • HY-122311

    SMTP-7

    Reactive Oxygen Species Neurological Disease Inflammation/Immunology
    Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS .
    Orniplabin
  • HY-N1306

    Bacterial Reactive Oxygen Species Apoptosis Infection Cancer
    Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against Staphylococcus aureus. Sideroxylin inhibits ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrial membrane, the generation of reactive oxygen species (ROS) .
    Sideroxylin
  • HY-161358

    FAK Apoptosis Cancer
    FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC50 value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. FAK-IN-20 can arrest the cell cycle in the G2/M phase and induce cell apoptosis by generating ROS .
    FAK-IN-20
  • HY-158016

    EGFR Apoptosis Cancer
    Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC50 of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC50 values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .
    Antiproliferative agent-49
  • HY-162488

    Fungal Infection
    Laccase-IN-3 (Compound 2b) is a laccase inhibitor (IC50 = 1.02= μM) with significant antifungal activity. Laccase-IN-3 shows superior inhibitory effect on Botryosphaeria dothidea (EC50 = 0.17 mg/L). Laccase-IN-3 effectively blocks the catalytic function of laccase by binding to its active center. Laccase-IN-3 also disrupts pathogen cell membrane integrity and increases ROS .
    Laccase-IN-3
  • HY-157437

    Cholinesterase (ChE) Reactive Oxygen Species Neurological Disease Inflammation/Immunology
    AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor with IC50s of 30 nM and 48 nM for human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), respectively. AChE/BChE-IN-16 exhibits a remarkable capacity to safeguard PC12 cells against H2O2-induced apoptosis and effectively suppresses the production of reactive oxygen species (ROS) .
    AChE/BChE-IN-16
  • HY-161966

    Apoptosis Reactive Oxygen Species VEGFR Cancer
    VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
    VEGFR-2-IN-52

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