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Home >> Signaling Pathways >> Tyrosine Kinase >> ROS

ROS(活性氧)

ROS is a proto-oncogenic receptor tyrosine kinase whose expression is tightly restricted during development. ROS kinase is one of the last two remaining orphan receptor tyrosine kinases. It is thought also that c-ROS gene may have a role in some cardiovascular diseases, and the fact that homozygous male mice targeted against c-ROS gene are healthy but infertile, has inspired researchers to think about ROS inhibition as a method for development of new male contraceptives. The new selective and potent inhibitors for ROS kinase, along with the development of new specific diagnostic methods for the detection of ROS fusion proteins, raises the importance of using these selective inhibitors for targeting ROS mutations as a new method for treatment of cancers harboring such genes.

Products for  ROS

  1. Cat.No. 产品名称 Information
  2. GC25000 (E/Z)-BCI (E/Z)-BCI (BCI, NSC 150117) is an inhibitor of dual specific phosphatase 1/6 (DUSP1/DUSP6) and mitogen-activated protein kinase with EC50 of 13.3 μM and 8.0 μM for DUSP6 and DUSP1 in cells, respectively. (E)-BCI induces apoptosis via generation of reactive oxygen species (ROS) and activation of intrinsic mitochondrial pathway in H1299 lung cancer cells.
  3. GC62633 GGTI-2154 GGTI-2154 是一种有效和选择性的 geranylgeranyltransferase I (GGTase I) 抑制剂，IC50 值为 21 nM。GGTI-2154 对 GGTase I 的选择性是 FTase (IC50=5600 nM) 的 200 倍以上。GGTI-2154 可用于癌症的研究。
  4. GC62351 Taletrectinib 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.
  5. GC38776 Ensulizole Ensulizole (PBSA), a water soluble sunscreen ingredient, is a sulfonated UV absorber which is characterized by intense UVB and partial UVA absorption. Ensulizole can damage the DNA through the generation of reactive oxygen species (ROS) upon UV or sunlight irradiation.
  6. GC36585 Merestinib dihydrochloride Merestinib dihydrochloride (LY2801653 dihydrochloride) 是一种II型ATP竞争性的 MET 抑制剂，Ki 值为 2 nM。
  7. GC36021 F-1 F-1 是一种有效的 ALK 和 ROS1 的双重抑制剂，抑制 ALK 的磷酸化及下游通路，对 ALKWT，ROS1WT，ALKL1196M 和 ALKG1202R 的 IC50 值分别为 2.1 nM，2.3 nM，1.3 nM 和 3.9 nM。
  8. GC43268 Cinnamtannin B-1 A polyphenol antioxidant
  9. GC41183 α-Carotene A precursor of vitamin A
  10. GC19362 Repotrectinib A multi-kinase inhibitor
  11. GC14476 Entrectinib A pan-Trk, ROS1, and ALK inhibitor
  12. GC14794 PF-06463922 An orally available inhibitor of ALK and ROS1
  13. GC12616 Crizotinib hydrochloride Crizotinib hydrochloride (PF-02341066 hydrochloride) 是一种具有口服生物利用度、选择性和 ATP 竞争性的双重 ALK 和 c-Met 抑制剂，IC50 分别为 20 和 8 nM。 Crizotinib hydrochloride (PF-02341066 hydrochloride) 在基于细胞的试验中抑制 NPM-ALK 的酪氨酸磷酸化和 c-Met 的酪氨酸磷酸化，IC50 分别为 24 和 11 nM。它也是一种 ROS 原癌基因 1 (ROS1) 抑制剂。 Crizotinib hydrochloride (PF-02341066 hydrochloride) 具有有效的肿瘤生长抑制作用。
  14. GC13136 (S)-Crizotinib An MTH1 inhibitor
  15. GC11057 LY2801653 A MET kinase inhibitor

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