上海源葉生物科技有限公司

主營產(chǎn)品: S30260異硫氰酸胍,30259鹽酸胍,嗜熱菌蛋白酶

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15921386130

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聯(lián)人:
何小姐
話:
86-021-61559134
機(jī):
15921386130
真:
86-021-55068248
址:
上海市松江區(qū)長塔路465號6幢
編:
200433
網(wǎng)址:
www.shyuanye.com
鋪:
http://m.true-witness.com/st191837/
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S80030
S80030
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更新時間:2024-07-03 18:57:29瀏覽次數(shù):114

聯(lián)系我們時請說明是化工儀器網(wǎng)上看到的信息,謝謝!

【簡單介紹】
提示:詳情請下載說明書
  • 提示:詳情請下載說明書。
  • 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(xiàn):
    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
  • 注意:部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的性,僅供客戶參考交流研究之用。
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