BMS-754807

• Catalog No.: S1124
• CAS Number: 1001350-96-4
• M. F.: C23H24FN9O
• M. W.: 461.4947632
• Storage: -20°C

SYNONYMS

• IUPAC 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
• IUPAC Traditional 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
• Synonyms: BMS754807

DATABASE IDS

• CAS Number: 1001350-96-4

PROPERTIES

• Target: IGF-1R
• Salt Data: Free Base
• Storage Condition: -20°C

DETAILS

Description (English)

Biological Activity:
BMS-754807 is an orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. [1] BMS-754807 inhibits the phosphorylation of IGF-1R (IC50 = 13nM) and the downstream targets Akt (IC50 = 22nM) and MAPK (IC50 = 13nM) in the IGF-Sal cell line with IC50 consistent with the antiproliferative IC50 (7 nM) in this cell line. [1] The protein binding for BMS-754807 ranges from of 98.5%in mouse plasma to 95.9%in human plasma. [1]BMS-754807 (Compound 9d) achieved complete tumor growth inhibition at the 6.25 mg/kg dose. This agent was identified with strong efficacy in the IGF-Sal tumor model with minimal weight loss at the upper dose. [1]

REFERENCES

• Mark D. Wittman et al. J. Med. Chem.2009,52(23):7360–7363