S80030
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- 公司名稱 上海源葉生物科技有限公司
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- 廠商性質(zhì) 生產(chǎn)廠家
- 更新時間 2024/7/3 18:57:29
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- 產(chǎn)品描述： BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases
- 靶點： IC50: 3.9 nM (c-Met), 1.1 nM (Axl), 1.8 nM (Ron), 4.3 nM (Tyro3)
- 體內(nèi)研究： Oral administration of BMS 777607 (6.25-50 mg/kg) significantly reduces tumor volumes of the GTL-16 human tumor xenografts in athymic mice with no observed toxicity. Administration of BMS 777607 (25 mg/kg/day) decreases the number of KHT lung tumor nodules (28.3%), improves the morphological hemorrhage, and significantly impairs the metastatic phenotype in the 6-8 week-old female C3H/HeJ mice injected with rodent fibrosarcoma KHT cells without apparent systemic toxicity compared to the control treatment. A low dose of BMS 777607 (10 mg/kg) also offers a mild but not significant inhibition of lung nodule formation compared to the vehicle control.
- 參考文獻：
1. Schroeder GM, et al. Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily. J Med Ch 2. Dai Y, et al. BMS-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. Mol Cancer Ther, 2010, 9(6), 1554-1561. 3. Dai Y, et al. Impact of the small molecule Met inhibitor BMS-777607 on the metastatic process in a rodent tumor model with constitutive c-Met activation. Clin Exp Metastasis, 2012, 29, 253-261.
- 溶解度： DMSO : ≥ 39 mg/mL (76.04 mM)
- 保存條件： -20℃
- 配置溶液濃度參考：
1mg 5mg 10mg 1 mM 1.95 ml 9.749 ml 19.497 ml 5 mM 0.39 ml 1.95 ml 3.899 ml 10 mM 0.195 ml 0.975 ml 1.95 ml 50 mM 0.039 ml 0.195 ml 0.39 ml
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