ROS Kinase
The transmembrane proto-oncogene receptor tyrosine kinase (RTK) ROS is one of the last two remaining orphan receptor tyrosine kinases. Its normal expression pattern is tightly spatiotemporally restricted during development. The ectopic expression, as well as the production of variable mutant forms of ROS kinase, has been reported in a number of cancers, such as glioblastoma multiforme, and non-small cell lung cancer, suggesting a role for ROS kinase in deriving such tumors. It is thought also that the c-ROS gene may have a role in some cardiovascular diseases, and the fact that homozygous male mice targeted against the c-ROS gene are healthy but infertile has inspired researchers to think about ROS inhibition as a method for the development of new male contraceptives.
ROS1 is a transmembrane receptor tyrosine kinase proto-oncogene that has been shown to have rearrangements with several genes in glioblastoma, non-small-cell lung cancer (NSCLC), and other neoplasms, including intrachromosomal fusion with GOPC due to microdeletions at 6q22.1. ROS1 fusion events are important findings in these tumors, as they are potentially targetable alterations with newer tyrosine kinase inhibitors.
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ROS Kinase Related Products (101)
Related Products (101)
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Antibodies (3)
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ROS kinases-IN-1
0 ImagesROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity.
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Entrectinib-d4
0 ImagesCat. No.: HY-12678SSynonyms: NMS-E628-d4; RXDX-101-d4Entrectinib-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.
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Entrectinib (Standard)
0 ImagesSynonyms: NMS-E628 (Standard); RXDX-101 (Standard)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.
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Crizotinib acetate
0 ImagesCat. No.: HY-50878BCAS No.: 877399-53-6Synonyms: PF-02341066 acetateCrizotinib (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.
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Taletrectinib free base
0 ImagesCat. No.: HY-131003ACAS No.: 1505514-27-1Synonyms: DS-6051b free base; AB-106 free base; IBI-344 free baseTaletrectinib (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.
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Fudotinib
0 ImagesCat. No.: HY-176942CAS No.: 2644645-39-4Synonyms: JYP0322Fudotinib (JYP0322) (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. Fudotinib selectively inhibits human wild-type ROS1 and human ROS1G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. Fudotinib inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. Fudotinib can be used for the research of non-small cell lung cancer (NSCLC).
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WY-135
0 ImagesCat. No.: HY-111416CAS No.: 2163060-83-9WY-135 is an ALK (IC50=1.4 nM) and ROS1 (IC50=1.1 nM) dual inhibitor.
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Lorlatinib acetate
0 ImagesCat. No.: HY-135509CAS No.: 1924207-18-0Synonyms: PF-06463922 acetateLorlatinib (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 ALKL1196M, respectively. Lorlatinib acetate targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALKL1196), 14-80 nM (ALKG1269A), 38-50 nM (ALK1151Tins), 77-113 nM (ALKG1202R), respectively.
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AChE/BChE/BACE-1-IN-1
0 ImagesCat. No.: HY-147658CAS No.: 1321361-13-0AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC50 values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential.
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Crizotinib-amide-PEG2-NH2
0 ImagesCat. No.: HY-176950CAS No.: 3048497-52-2Crizotinib-amide-PEG2-NH2 is a MET ligand (HY-50878) linker conjugate. Crizotinib-amide-PEG2-NH2 can be used for synthesis of MET degrader OZD-MET 01 (HY-177893).
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DHODH-IN-33
0 ImagesCat. No.: HY-179531CAS No.: 3026839-88-0DHODH-IN-33 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor with potent activity against A549 (IC50 = 5.22 μM) and 5637 (IC50 = 3.03 μM). DHODH-IN-33 induces autophagy-dependent ferroptosis (mitochondrial dysfunction, lipid peroxidation, and ROS accumulation) with no notable toxicity in vivo. DHODH-IN-33 exerts anti-cancer effect by promoting the autophagy-dependent degradation of DHODH. DHODH-IN-33 can be used for non-small cell lung cancer and bladder cancer.
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Antitumor agent-60
0 ImagesCat. No.: HY-146432CAS No.: 865784-65-2Antitumor agent-60 (compound 20) is a potent antitumor agent, targeting RAS-RAF signaling pathway and binding to CRAF with a Kd value of 3.93 μM. Antitumor agent-60 induces apoptosis by blocking cell cycle at G2/M phase. Antitumor agent-60 enhances the level of p53 and ROS. Antitumor agent-60 causes oval and irregular nucleus in cancer cells. Antitumor agent-60 can suppress the growth of tumor to some extent in A549 xenograft model.
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Antibacterial agent 69
0 ImagesCat. No.: HY-144252CAS No.: 2915755-61-0Antimicrobial agent 69 is a novel structural antimicrobial regulator and has been used to fight deadly multidrug-resistant bacterial infections, and its MICs value is 2.978 μM.
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HS-291
0 ImagesCat. No.: HY-157084HS-291 is a HtpG inhibitor of Borrelia burgdorferi (Bb). HS-291 contains BX-2819 (high affinity for Bb HtpG), PEG linker, and Verteporfin (HY-B0146) (a photoactive toxin).HS-291 produces reactive oxygen species under light activation to oxidize HtpG and a discrete protein subset near chaperone proteins and can quickly and irreversibly inactivate Bb.
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Crizotinib-d9 hydrochloride
0 ImagesCat. No.: HY-50878ASSynonyms: PF-02341066-d9 hydrochlorideCrizotinib-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.
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ALK/ROS1-IN-1
0 ImagesCat. No.: HY-130794CAS No.: 2365497-07-8ALK/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.
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ROS1-IN-1
0 ImagesCat. No.: HY-150974CAS No.: 2883232-34-4ROS1-IN-1 (Compound 31) is a potent and selective ROS1 kinase inhibitor with an IC50 of 0.097 μM.
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Antitumor agent-55
0 ImagesCat. No.: HY-146038CAS No.: 2522594-49-4Antitumor agent-55 (compound 5q) is a potent antitumor agent. Antitumor agent-55 effectively inhibits PC3, with an IC50 of 0.91 μM. Antitumor agent-55 effectively inhibits the colony formation, suppresses the cell migration in PC3. Antitumor agent-55 induces G1/S phase arrest and apoptosis in PC3.
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CM-728
0 ImagesCat. No.: HY-170488CAS No.: 2925046-28-0CM-728 is a oxazepine-naphthoquinone that has cytotoxic and bactericidal effect. CM-728 is a human peroxiredoxin-1 inhibitor. CM-728 is an oxidative stressor that affects mitochondrial function.
