Product Name: BMS-754807

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CAT#: A-1013


  Synonym:BMS754807

BMS-754807 Chemical Structure
BMS-754807 chemical structure


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IUPAC/Chemical name: (S)-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.

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Biological Activity

BMS-754807 is an orally bioavailable human IGF-1R inhibitor currently in Phase I/II clinical trials for the treatment of advanced metastatic solid tumors.

BMS-754807 is an orally bioavailable antagonist of human insulin-like growth factor type I receptor (IGF-1R) with potential antineoplastic activity. IGF-1R antagonist BMS-7548077 binds to IGF-1R, preventing IGF-1 ligand binding and activation of IGF-1R-mediated signaling pathways; inhibition of IGF-1R-mediated signaling pathways may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-1R is a receptor tyrosine kinase expressed on most tumor cells and is involved in mitogenesis, angiogenesis, and tumor cell survival.

Technical Data

Formula: C23H24FN9O
MW: 461.51

CAS#: 1001350-96-4
Optical purity: 100% by chiral HPLC
Chemical Purity: >99% by HPLC
Storage Conditions :Room temperature, or -20ºC for 2 year.
BMS-754807 MSDS BMS-754807 CoA

Reference
1: Hou X, Huang F, Macedo LF, Harrington SC, Reeves KA, Greer A, Finckenstein FG, Brodie A, Gottardis MM, Carboni JM, Haluska P. Dual IGF-1R/InsR inhibitor BMS-754807 synergizes with hormonal agents in treatment of estrogen-dependent breast cancer. Cancer Res. 2011 Dec 15;71(24):7597-607. Epub 2011 Oct 31. PubMed PMID: 22042792.
2: Scagliotti GV, Novello S. The role of the insulin-like growth factor signaling pathway in non-small cell lung cancer and other solid tumors. Cancer Treat Rev. 2011 Sep 8. [Epub ahead of print] PubMed PMID: 21907495.
3: King ER, Wong KK. Insulin-like growth factor: current concepts and new developments in cancer therapy. Recent Pat Anticancer Drug Discov. 2012 Jan;7(1):14-30. PubMed PMID: 21875414.
4: Kolb EA, Gorlick R, Lock R, Carol H, Morton CL, Keir ST, Reynolds CP, Kang MH, Maris JM, Billups C, Smith MA, Houghton PJ. Initial testing (stage 1) of the IGF-1 receptor inhibitor BMS-754807 by the pediatric preclinical testing program. Pediatr Blood Cancer. 2011 Apr;56(4):595-603. doi: 10.1002/pbc.22741. Epub 2010 Dec 22. PubMed PMID: 21298745.



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