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AC480 (BMS-599626)

In stock
Catalog No.
A2822
HER1/2 inhibitor,selective and efficacious
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$273.00
In stock
5mg
$120.00
In stock
25mg
$380.00
In stock
100mg
$700.00
In stock

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Email: [email protected]

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Background

AC480 (BMS-599626) is a potent, selective inhibitor of human epidermal growth factor receptor (HER) that inhibits HER1 and HER2 with IC values of 20 nM and 30 nM, respectively. AC480 has been proved to inhibit HER1 in an ATP-competitive manner. On the contrary, AC480 has shown to be an ATP noncompetitive inhibitor of HER2 [1]

AC480 inhibited the proliferation of Sal2 cells derived from a transgenic mouse tumor, breast tumor and gastric carcinoma cell lines, GEO colon tumor cells, non–small-cell lung tumor cells line via HER1 and/or HER2 signalings [1].

AC480 by oral administration has been demonstrated to suppress the growth of Sal2 tumor, GEO xenograft tumor, KPL-4 and BT474 breast tumors, N87 gastric tumor, A549 and L2987 non–small-cell lung tumors in nude mice [1].

References:
[1] Wong TW1, Lee FY, Yu C, Luo FR, Oppenheimer S, Zhang H, Smykla RA, Mastalerz H, Fink BE, Hunt JT,Gavai AV, Vite GD. Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006 Oct 15;12(20 Pt 1):6186-93.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt567.01
Cas No.714971-09-2
FormulaC27H27FN8O3.HCl
Solubility≥28.35mg/mL in DMSO
Chemical Name[(3S)-morpholin-3-yl]methyl N-[4-[[1-[(3-fluorophenyl)methyl]indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamate
SDFDownload SDF
Canonical SMILESCC1=C2C(=NC=NN2C=C1NC(=O)OCC3COCCN3)NC4=CC5=C(C=C4)N(N=C5)CC6=CC(=CC=C6)F
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description AC480 is a selective and efficacious inhibitor of HER1 and HER2 with IC50 values of 20 nM and 30 nM, respectively.
Targets HER1 HER2        
IC50 20 nM 30 nM        

Quality Control

Quality Control & MSDS

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Chemical structure

AC480 (BMS-599626)