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.