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ONO-7475
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ONO-7475图片
CAS NO:1646839-59-9
包装与价格:
包装价格(元)
10mM 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议

产品介绍
ONO-7475 是一种有效的、选择性的、具有口服活性的 Axl/Mer 抑制剂,IC50 值分别为 0.7 nM 和 1.0 nM。 ONO-7475 使过表达 AXL 的 EGFR 突变 NSCLC 细胞对 EGFR-TKI 敏感,抑制耐受细胞的出现和维持。 ONO-7475 与 Osimertinib 联合为 EGFR 突变的非小细胞肺癌 (NSCLC) 的研究提供了光明的前景。
Cas No.1646839-59-9
化学名N-[5-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-pyridinyl]-1,2,5,6,7,8-hexahydro-2,5-dioxo-1-phenyl-3-quinolinecarboxamide
Canonical SMILESO=C(C1=CC2=C(N(C3=CC=CC=C3)C1=O)CCCC2=O)NC4=NC=C(OC5=CC=NC6=CC(OC)=C(OC)C=C56)C=C4
分子式C32H26N4O6
分子量562.58
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.