ROS

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.

Targets for ROS

Products for ROS

Cat.No. Product Name Information
GC41183 α-Carotene
α-Carotene is a precursor of vitamin A that has been found in various fruits and vegetables.
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.
GC13136 (S)-Crizotinib Potent MTH1 inhibitor
GC43268 Cinnamtannin B-1 Cinnamtannin B-1 is a proanthocyanidin polyphenol originally isolated from cinnamon bark that has antioxidant properties.
GC12616 Crizotinib hydrochloride
inhibitor of the c-Met kinase and the NPM-ALK
GC38776 Ensulizole Ensulizole is a sulfonated UV absorber and can intense UVB and partial UVA absorption.
GC14476 Entrectinib Orally active inhibitor of ALK kinase
GC36021 F-1 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 ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively.
GC62633 GGTI-2154 GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.
GC11057 LY2801653 A MET kinase inhibitor
GC36585 Merestinib dihydrochloride 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).
GC14794 PF-06463922 PF-06463922 (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor. PF-06463922 has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALKL1196M, respectively. PF-06463922 has anticancer activity.
GC19362 Repotrectinib TPX-0005 is a potent ALK/ROS1/TRK inhibitor, with IC50 of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively.
GC62351 Taletrectinib 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.