ONO-7475 (Synonyms: ONO-7475) |
رقم الكتالوجGC18416 |
ONO-7475 هو مثبط Axl / Mer فعال وانتقائي وفعال عن طريق الفم بقيم IC50 تبلغ 0.7 نانومتر و 1.0 نانومتر على التوالييعمل ONO-7475 على توعية خلايا NSCLC المتغيرة بشكل مفرط في EGFR إلى EGFR-TKIs ، ويثبط ظهور الخلايا المتسامحة والحفاظ عليهايوفر اتحاد ONO-7475 مع Osimertinib وعدًا مشرقًا لدراسة سرطان الرئة ذو الخلايا غير الصغيرة المتحول إلى EGFR (NSCLC)
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Cas No.: 1646839-59-9
Sample solution is provided at 25 µL, 10mM.
ONO-7475 is a potent and orally active Axl/Mer inhibitor. ONO-7475 targets and binds to both Axl and Mer, and prevents their activity. This blocks Axl- and Mer-mediated signal transduction pathways, and inhibits proliferation and migration of Axl- and Mer-overexpressing tumor cells. Axl and Mer, both members of the TAM (Tyro3, Axl and Mer) family of RTKs, are overexpressed by many tumor cell types. They play key roles in tumor cell proliferation, survival, invasion, angiogenesis and metastasis, and their expression is associated with drug resistance and poor prognosis
Reference:
[1]: Okura N, Nishioka N, Yamada T, Taniguchi H, Tanimura K, Katayama Y, Yoshimura A, Watanabe S, Kikuchi T, Shiotsu S, Kitazaki T, Nishiyama A, Iwasaku M, Kaneko Y, Uchino J, Uehara H, Horinaka M, Sakai T, Tanaka K, Kozaki R, Yano S, Takayama K. ONO-7475, a Novel AXL Inhibitor, Suppresses the Adaptive Resistance to Initial EGFR-TKI Treatment in EGFR-Mutated Non-Small Lung Cancer. Clin Cancer Res. 2020 Jan 17. doi: 10.1158/1078-0432.CCR-19-2321. Epub ahead of print. PMID: 31953310.
[2]: Ruvolo PP, Ma H, Ruvolo VR, Zhang X, Mu H, Schober W, Hernandez I, Gallardo M, Khoury JD, Cortes J, Andreeff M, Post SM. Anexelekto/MER tyrosine kinase inhibitor ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells by diverse mechanisms. Haematologica. 2017 Dec;102(12):2048-2057. doi: 10.3324/haematol.2017.168856. Epub 2017 Sep 14. PMID: 28912176; PMCID: PMC5709104.
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