BMS-599626|714971-09-2|AC480|AC-480|BMS 599626|(S)-Morpholin-3-ylmethyl (4-((1-(3-fluorobenzyl)-1H-indazol-5-yl)amino)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl)carbamate|AC480 (BMS-599626)|BMS599626|CHEMBL1645462|BMS-599626 (AC480)|2252724U5N|Carbamic ac
Specifications & Purity
Moligand™, ≥98%
Biochemical and Physiological Mechanisms
BMS-599626 is a potent inhbitor of human epidermal growth factor receptors 1 and 2 (HER1 and HER2, IC50 = 20 and 30 nM, respectively). BMS599626 inhibits proliferation of several HER-expressing cancer cell lines, including HER2-overexpressing breast cance
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Receptor protein-tyrosine kinase erbB-4 inhibitor
Product Description
AC480 (BMS-599626) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, >100-fold to VEGFR2, c-Kit, Lck, MET etc.
Product Properties
ALogP
2.8
Associated Targets
C7orf77Tdark Uncharacterized protein C7orf77 0 Activities
1.Gavai AV, Fink BE, Fairfax DJ, Martin GS, Rossiter LM, Holst CL, Kim SH, Leavitt KJ, Mastalerz H, Han WC et al.. (2009) Discovery and preclinical evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic acid, (3S)-3-morpholinylmethyl ester (BMS-599626), a selective and orally efficacious inhibitor of human epidermal growth factor receptor 1 and 2 kinases.. J Med Chem, 52 (21):(6527-30). [PMID:19821562]
2.Soria JC, Cortes J, Massard C, Armand JP, De Andreis D, Ropert S, Lopez E, Catteau A, James J, Marier JF et al.. (2012) Phase I safety, pharmacokinetic and pharmacodynamic trial of BMS-599626 (AC480), an oral pan-HER receptor tyrosine kinase inhibitor, in patients with advanced solid tumors.. Ann Oncol, 23 (2):(463-71). [PMID:21576284]
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A2210095