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BMS-754807

CAS No. : 1001350-96-4

MCE 国际站：BMS-754807

产品活性：BMS-754807 是有效、可逆的 IGF-1R/IR 抑制剂，其 IC₅₀ 值分别为 1.8 和 1.7 nM，K_i 值均小于 2 nM。BMS-754807 同时也抑制 Met，RON，TrkA，TrkB，AurA 和 AurB 的活性，IC₅₀ 值分别为 6，44，7，4，9 和 25 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：IGF-1R  |  Insulin Receptor

In Vitro: BMS-754807 effectively inhibits the growth of a broad range of human tumor cell lines with IC₅₀ values of ranging from 5 to 365 nM. BMS-754807 also inhibits the proliferation of human rhabdomyosarcoma tumor cells Rh41 and human colon carcinoma Geo with IC₅₀s of 7 and 5 nM, respectively. BMS-754807 shows inhibitory activity in the proliferation of Rh41 cells with IC₅₀ of 5 nM. BMS-754807 inhibits the phosphorylation of IGF-1R (IC₅₀=13 nM) and the downstream targets Akt (IC₅₀=22 nM) and MAPK (IC₅₀=13 nM) in the IGF-Sal cell line with IC₅₀ consistent with the antiproliferative IC₅₀ (7 nM) in this cell line. BMS-754807 shows a median EC₅₀ value of 0.62 μM against the PPTP cell lines. The median EC₅₀ for the four Ewing sarcoma cell lines is less than that for the remaining PPTP cell lines (0.19 μM vs. 0.78 μM, P=0.0470). BMS-754807 (0.25 and 0.5 μM) reduces the activated IGF-IR/IR (pIGF-IR/IR), causes a concurrent decrease in phosphorylated AKT in both lung cancer cell lines. BMS-754807 (0.5 μM) also reduces wound closure of lung cancer cells and reduces the ERK phosphorylation. BMS-754807 reduces cell viability in both A549 and NCI-H358 cells, with IC₅₀ of 1.08 μM and 76 μM, respectively.

In Vivo: 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.

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