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ROS Kinase

Proto-oncogene tyrosine-protein kinase ROS is an enzyme that in humans is encoded by the ROS1 gene. ROS Kinase is highly expressed in a variety of tumor cell lines, belongs to the sevenless subfamily of tyrosine kinase insulin receptor genes. The protein encoded by this gene is a type I integral membrane protein with tyrosine kinase activity. The protein may function as a growth or differentiation factor receptor.

  • ROS kinases-IN-2
    T74671687576-28-9
    ROS kinases-IN-2 is a potent ROS kinase inhibitor with an inhibition rate of 21.53% measured at 10 μM.ROS kinases-IN-2 has potential anticancer activity and can be used to study abnormal cell growth.
    • $195
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  • Repotrectinib
    T40711802220-02-5
    Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.
    • $45
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  • Salvigenin
    TMS174319103-54-9
    Salvigenin is a potent hMAO-A inhibitor, has neuroprotective, antitumor and immunomodulatory effects.
    • $65
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  • Crizotinib
    T1661877399-52-5
    Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor.
    • $46
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  • Lorlatinib
    T30611454846-35-5
    Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.
    • $35
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    TargetMol | Citations Cited
  • Entrectinib
    T36781108743-60-7
    Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.
    • $35
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  • F-1
    T112542244775-31-1
    F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways.
    • $111
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  • ROS kinases-IN-1
    T60220370096-57-4
    ROS kinases-IN-1 is a ROS tyrosine kinase inhibitor with IC50 value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity.
    • $93
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  • ROS-generating agent 1
    T777622369030-41-9
    Ros-generating agent 1 has anticancer activity and generates ROS by covalently modifying Sec-498 residues of TrxR. ROS-generating agent 1 reduces intracellular TrxR protein levels and promotes ROs-dependent apoptosis and ferroptosis in NCI-H460 cells.
    • $31
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  • Anti-inflammatory agent 64
    T83048
    Anti-inflammatory agent 64 (compound 4b) exhibits antioxidant and anti-inflammatory activities, effectively inhibiting the secretion of IL-6 and TNF-α while also reducing paw edema [1] in both in vitro and in vivo studies.
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  • Uniconazole
    T2148283657-22-1
    Uniconazole is a plant growth regulator that inhibit cytochrome P450 707As (Ki=68 nM). CYP707As is a major ABA catabolic enzyme that catabolize Abscisic acid, accordingly suppress gibberellin and sterol biosynthesis.
    • $34
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  • Taletrectinib free base
    T389951505514-27-1
    Taletrectinib free base (AB-106 free base) is a novel potent, selective and orally active ROS1/NTRK inhibitor.Taletrectinib free base has potent inhibitory effects on recombinant ROS1, NTRK1, NTRK2, and NTRK3, with IC50s of 0.207, 0.622, 2.28 and 0.98 nM, respectively, Taletrectinib free base also inhibited ROS1 G2032R and other Crizotinib-resistant ROS1 mutations.
    • $65
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  • HS-291
    T82171
    HS-291 is a HtpG inhibitor targeting Borrelia burgdorferi (Bb), composed of BX-2819 (high affinity for Bb HtpG), a PEG linker, and Verteporfin (a photoactive toxin). Upon light activation, HS-291 generates reactive oxygen species that oxidize HtpG and selectively inactivate a subset of proteins in proximity to chaperones, facilitating the rapid and irreversible inactivation of Bb [1].
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  • APG-2449
    T793632196186-84-0
    APG-2449 is an orally active inhibitor targeting ALK, ROS1, and FAK, demonstrating antitumor efficacy in mouse models of non-small cell lung cancer (NSCLC) [1].
    • $1,520
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  • Taletrectinib
    T223181505515-69-4
    Taletrectinib (AB-106) is a new-generation selective inhibitor of ROS1/NTRK including ROS1,NTRK1,NTRK2 and NTRK3 with IC50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM, respectively.
    • $68
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  • Methyl 12-methyltridecanoate
    T791595129-58-8
    Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride), a biosurfactant derived from Brevibacterium casei LS14, enhances the biocompatibility of functionalized silver nanoparticles in vivo [1].
    • $143
    35 days
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  • Zidesamtinib
    T729532739829-00-4
    Zidesamtinib (NVL-520) is an orally active, selective, potent, and blood-brain-barrier-crossing inhibitor of ROS1 fusion and resistance mutations, inhibits ROS1 and ROS1 G2032R, and can be used in the study of non-small-cell lung cancer and solid tumors.
    • $196
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  • Merestinib
    T34551206799-15-6
    Merestinib (LY2801653) is an orally available, small molecule inhibitor of the proto-oncogene c-Met (Ki: 2 nM) with potential antineoplastic activity. Merestinib electively binds to c-Met, thereby inhibiting c-Met phosphorylation and disrupting c-Met signal transduction pathways. This may induce cell death in tumor cells overexpressing c-Met protein or expressing the constitutively activated c-Met protein.
    • $45
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  • Crizotinib hydrochloride
    T83991415560-69-8
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met(IC50s of 20 and 8 nM)
    • $31
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  • Iruplinalkib
    T640281854943-32-0
    Iruplinalkib (WX-0593) is an orally active, selective and potent ALK and ROS1 tyrosine kinase inhibitor with anticancer activity for use in the study of non-small cell lung cancer.
      7-10 days
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