Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.
ターゲット&IC50 | TrkA:7.4 nM, TrkB:4.1 nM, IGF-1R:1.8 nM, MET:5.6 nM, Insulin receptor:1.7 nM |
In vitro | MS-754807 (6.25 mg/kg) achieved complete tumor growth inhibition in a transgenic-derived IGF-Sal tumor model in mice, while simultaneously inhibiting associated pIGF-1R and pAKT. In nude mice with IGF-1R-Sal tumors, BMS-754807 (12.5 mg/kg, orally) inhibited tumor and serum IGF-1R phosphorylation. At a dose of 25 mg/kg, BMS-754807 significantly inhibited tumor growth in mouse models carrying KT-5 (Wilms), KT-14 (rhabdoid), Rh28 (rhabdomyosarcoma), and OS-1 xenografts. Furthermore, BMS-754807 effectively suppressed tumor growth across a selection of epithelial (IGF-1R-Sal, GEO, and Colo205), hematopoietic (JJN3), and mesenchymal (RD1 and Rh41) xenograft models, with tumor growth inhibition rates ranging from 53% to 115%. |
In vivo | BMS-754807 inhibits the phosphorylation of IGF-1R in IGF-1R-Sal cells, Rh41, and Geo with IC50 values of 13 nM, 6 nM, and 21 nM, respectively. It similarly inhibits the phosphorylation of Akt in these cells, with IC50 values of 22 nM, 13 nM, and 16 nM. Additionally, BMS-754807 induces apoptosis in Rh41 cells and suppresses the proliferation of IGF-1R-Sal and Rh41 cells, with IC50 values of 7 nM and 5 nM, respectively. In the pediatric preclinical testing program (PPTP), BMS-754807 exhibited activity across 23 cell lines with an average EC50 value of 0.62 μM, covering a range of cell types including mesenchymal (Ewing's, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreatic, colon, and gastric cancers), and hematopoietic stem cells (multiple myeloma and leukemia), with IC50 values spanning from 5 nM to 365 nM. |
分子量 | 461.49 |
分子式 | C23H24FN9O |
CAS No. | 1001350-96-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: 85 mg/mL (184.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 85 mg/mL (184.2 mM)
You can also refer to dose conversion for different animals. 詳細
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
BMS-754807 1001350-96-4 Tyrosine Kinase/Adaptors c-Met/HGFR Trk receptor IGF-1R Insulin Receptor BMS 754807 BMS754807 inhibit Inhibitor inhibitor