BMS-754807
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively[1].
Product Specifications
CAS Number
1001350-96-4
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
IGF-1R; Insulin Receptor
Type
Reference compound
Related Pathways
Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer; Endocrinology
Assay Protocol
https://www.medchemexpress.com/BMS-754807.html
Purity
99.42
Solubility
DMSO : ≥ 100 mg/mL
Smiles
FC1=CC=C(NC([C@@]2(C)N(C(N=C3NC4=NNC(C5CC5)=C4)=NN6C3=CC=C6)CCC2)=O)C=N1
Molecular Formula
C23H24FN9O
Molecular Weight
461.49
Precautions
H302, H315, H319, H335
References & Citations
[1]Carboni JM, et al. BMS-754807, a small molecule inhibitor of IGF-1R/IR. Mol Cancer Ther, 2009, 8 (12), 3341-3349.|[2]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.|[3]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.|[4]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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 2
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