BMS-754807
BMS-754807 (CAS 1001350-96-4) is a small molecule inhibitor targeting insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR). Acting as an ATP-competitive antagonist, it directly interferes with the catalytic kinase domains of IGF-1R/IR, thereby disrupting their enzymatic activities. In vitro studies demonstrated potent antiproliferative activity against various cancer cell lines, including mesenchymal, hematopoietic, and epithelial tumors (IC50 ranging from 5 to 365 nmol/L). Furthermore, evidence from apoptosis assays in human rhabdomyosarcoma cells indicates BMS-754807 can induce apoptosis, characterized by increased caspase cleavage and poly(ADP-ribose) polymerase (PARP) fragmentation. This compound is primarily applied in oncology research aimed at elucidating IGF-1R/IR signaling pathways.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 461.49 |
| Cas No. | 1001350-96-4 |
| Formula | C23H24FN9O |
| Solubility | ≥23.05 mg/mL in DMSO; insoluble in H2O; ≥27.75 mg/mL in EtOH |
| Chemical Name | (2S)-1-[4-[(5-cyclopropyl-1H-pyrazol-3-yl)amino]pyrrolo[2,1-f][1,2,4]triazin-2-yl]-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | CC1(CCCN1C2=NN3C=CC=C3C(=N2)NC4=NNC(=C4)C5CC5)C(=O)NC6=CN=C(C=C6)F |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment: [1] | |
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Cell lines |
IGF-1R-Sal, Rh41 and Geo cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
1 μM, (72 hours for cell proliferation inhibition; 1 hour for phosphorylation inhibition |
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Applications |
Cell proliferation was evaluated by incorporation of 3H-thymidine into DNA after exposure of cells to BMS-754807 with concentrations from 0.1 to 1000 nM. BMS-754807 inhibited cell proliferation with IC50 values of 7, 5 and 365 nM for IGF-1R-Sal, Rh41 and Geo cells, respectively. The IC50 values for inhibition of the pIGF-1R by BMS-754807 and downstream components (e.g., pAkt) were very similar. In contrast, there was greater inhibition against pMAPK in IGF-1R-Sal cells compared with Rh41 and Geo, indicating that additional compensatory pathways such as EGFR might be important in driving signals in both Rh41 and Geo cell types. |
| Animal experiment : [1] | |
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Animal models |
Nude mice bearing various tumor xenografts (Sal-IGF, GEO, Colo205, JJN3, Rh41 or RD1) |
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Dosage form |
Oral administration, 0.01 mL/g of body weight |
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Applications |
BMS-754807 inhibited 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%. In the highly sensitive Rh41 rhabdomyosarcoma, BMS-754807 was effective at a dose level of 3.125 mg/kg twice daily and as low as 6.25 mg/kg once daily. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1] Carboni J M, Wittman M, Yang Z, et al. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Molecular Cancer Therapeutics, 2009, 8(12): 3341-3349. | |
| Description | BMS-754807 is a potent and selective inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor family kinase (InsR) with IC50 values of 1.8 nM and 1.7 nM, respectively. | |||||
| Targets | IGF-1R | InsR | ||||
| IC50 | 1.8 nM | 1.7 nM | ||||
Quality Control & MSDS
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Chemical structure
