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S80003

BMS-754807

源葉(MedMol) 99%
  • 英文名:
  • BMS-754807
  • 別名:
  • (S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
  • CAS號:
  • 1001350-96-4
  • 分子式:
  • C23H24FN9O
  • 分子量:
  • 461.49
  • 核磁/質(zhì)譜:
品牌貨號產(chǎn)品規(guī)格價(jià)格(RMB) 庫存(上海) 北京 武漢 南京 數(shù)量計(jì)量單位 加入購物車...
源葉(MedMol) S80003-5mg 99% ¥345.00元 3 - - - EA 加入購物車
源葉(MedMol) S80003-10mg 99% ¥620.00元 3 - - - EA 加入購物車
源葉(MedMol) S80003-50mg 99% ¥2250.00元 7 - - - EA 加入購物車
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產(chǎn)品介紹

參考文獻(xiàn)

質(zhì)檢證書(COA)

摩爾濃度計(jì)算器

相關(guān)產(chǎn)品

  • 提示:詳情請下載說明書。
  • 產(chǎn)品描述: BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively
  • 靶點(diǎn): IC50: 1.7 nM (IR), 1.8 nM (IGF-1R), 4 nM (TrkB), 6 nM (Met), 7 nM (TrkA), 9 nM (AurA), 25 nM (AurB), 44 nM (RON);Trkreceptor;c-Met/HGFR;IGF-1R
  • 體內(nèi)研究:
    BMS-754807 (3.125 and 12.5 mg/kg, p.o.) inhibits tumor growth in IGF-1R-Sal tumor-bearing nude mice. BMS-754807 inhibits tumor growth in a selected group of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft tumor models with TGI ranging from 53% to 115%. BMS-754807 is effective at a dose level of 3.125 mg/kg twice daily and as low as 6.25 mg/kg once daily, in the highly sensitive Rh41 rhabdomyosarcoma. BMS-754807 (25 mg/kg) also shows synergy when combined with targeted agents in human tumor cell lines and human xenograft models. Furthmore, BMS-754807 is active at doses from 3 mg/kg upward in the IGF-Sal tumor model. BMS-754807 (25 mg/kg, p.o.) induces significant differences in EFS distribution compared to controls in 18 of 32 evaluable solid tumor xenografts (56%) tested, but in none of the ALL xenografts studied
  • 參考文獻(xiàn):
    1. Carboni JM, et al. BMS-754807, a small molecule inhibitor of IGF-1R/IR. Mol Cancer Ther, 2009, 8(12), 3341-3349. 2. Franks SE, et al. BMS-754807 is cytotoxic to non-small cell lung cancer cells and enhances the effects of platinum chemotherapeutics in the human lung cancer cell line A549. BMC Res Notes. 2016 Mar 1;9:134. 3. Wittman MD, et al. Discovery of a 2,4-disubstituted pyrrolo[1,2-f][1,2,4]triazine inhibitor (BMS-754807) of IGF-1R kinase in clinical development. J Med Chem, 2009, 52(23), 7360-7363. 4. Kolb EA, et al. Initial testing (stage 1) of the IGF-1 receptor inhibitor BMS-754807 by the pediatric preclinical testing program. Pediatr Blood Cancer, 2011, 56(4), 595-603.
  • 溶解性: DMSO  :  ≥  100  mg/mL  (216.69  mM)
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 2.167 ml 10.834 ml 21.669 ml
    5 mM 0.433 ml 2.167 ml 4.334 ml
    10 mM 0.217 ml 1.083 ml 2.167 ml
    50 mM 0.043 ml 0.217 ml 0.433 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權(quán)威性,僅供客戶參考交流研究之用。
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質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)


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