BMS-754807 is a potent and reversible inhibitor of the type-1 insulin-like growth factor receptor family kinases (Ki, <2 nmol/L). BMS-754807 effectively inhibits the growth of a broad range of human tumor types in vitro, including mesenchymal, epithelial and hematopoietic tumor cell lines (IC50, 5-365 nmol/L). In vitro, BMS-754807 showed a median EC(50) value of 0.62 μM against the PPTP cell lines. BMS-754807 caused apoptosis in a human rhabdomyosarcoma cell line, Rh41, as shown by an accumulation of the sub-G1 fraction, as well as by an increase in poly ADP ribose polymerase and Caspase 3 cleavage. BMS-754807 is active in vivo in multiple xenograft tumor models with tumor growth inhibition ranging from 53% to 115% and at a minimum effective dose of as low as 6.25 mg/kg dosed orally daily. BMS-754807 is currently in phase I development for the treatment of a variety of human cancers.
Neuroreport. 2019 May 22;30(8):580-585.
Insulin attenuates epileptiform discharge-induced oxidative stress by increasing zinc-α2-glycoprotein in primary cultured cortical neurons.
BMS-754807 purchased from AbMole
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Source | Int J Mol Sci (2017). Figure 5. BMS-754807 |
| Method | IGF1R/IR and AR antagonists | |
| Cell Lines | TNBC cell | |
| Concentrations | 20 μM | |
| Incubation Time | 48 h | |
| Results | In this panel of TNBC cell lines, inhibition by BMS-754807 consistently induced cell death. These data suggest that inhibitors targeting IGF1R/IR homo- or heterodimers can prevent TNBC tumor growth. |
| Molecular Weight | 461.49 |
| Formula | C23H24FN9O |
| CAS Number | 1001350-96-4 |
| Solubility (25°C) | DMSO 72 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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