BMS-754807 Inhibitor CAS No. 1001350-96-4

Cat. No.	Name	Size	Price
KI2861	BMS-754807	5 mg	$288
	BMS-754807	10 mg	$432
	BMS-754807	50 mg	$1232
	BMS-754807	200 mg	$3312

Chemical Characteristic

Product Name	BMS-754807
Synonyms	BMS754807
CAS No.	1001350-96-4
Molecular Weight	461.51
Formula	C₂₃H₂₄FN₉O
Chemical Name	(S)-1-(4-(5-cyclopropyl-1H-pyrazol-3-ylamino)pyrrolo[1,2-f][1,2,4]triazin-2-yl)-N-(6-fluoropyridin-3-yl)-2-methylpyrrolidine-2-carboxamide
Smiles	N1([C@@](CCC1)(C(=O)Nc1cnc(cc1)F)C)c1nn2c(c(n1)Nc1n[nH]c(c1)C1CC1)ccc2
Chemical Structure

Biological activities

BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR. The IC50s of BMS-754807 against IGF-1R and InsR are 1.8 and 1.7 nM, respectively. In vitro, BMS-754807 effectively inhibits the growth of a variety of human tumor types, including mesenchymal (Ewing's, rhabdomyosarcoma, neuroblastoma, and liposarcoma), epithelial (breast, lung, pancreatic, colon, gastric), and hematopoietic (multiple myeloma and leukemia) tumor cell lines with IC50s ranging from 5 to 365 nM. In vivo, BMS-754807 treatment shows potent tumor growth inhibition with TGI values ranging from 53% to 115% in multiple (epithelial, mesenchymal, and hematopoietic) xenograft tumor models and has a minimum effective dose of as low as 6.25 mg/kg dosed orally daily.^[1]

Protocols

In vitro: Prior to use, BMS-754807 is dissolved in DMSO.^[2]

References

[1] Carboni JM, et al. BMS-754807, a small molecule inhibitor of insulin-like growth factor-1R/IR. Mol Cancer Ther. 2009, 8(12): 3341-3349. [2] Litzenburger BC, et al. High IGF-IR activity in triple-negative breast cancer cell lines and tumorgrafts correlates with sensitivity to anti-IGF-IR therapy. Clin Cancer Res. 2011, 17(8): 2314-2327.

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