S80003
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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 2024/7/2 19:54:37
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- 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： 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)
- 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：
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.
- 溶解度： 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
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