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BMS-599626 Hydrochloride

Catalog No.
A3252
EGFR/HER2 inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
5mg
$126.00
Ship with 10-15 days
50mg
$628.00
Ship with 10-15 days
100mg
$1,046.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

BMS-599626 is a selective inhibitor of HER1 and HER2 with IC50 value of 22 nM and 32 nM, respectively [1].
HER (human epidermal growth factor receptor) is a member of EGFR/ErbB family and plays an important role in transduction of cell proliferation and differentiation. It has been reported that abbrent expression of HER is correlated with cancer and HER inhibition is being regarded as a promising strategy for cancer treatment [1].
BMS-599626 is a potent HER inhibitor and has the higher inhibition ability than the other reported inhibitors. When tested with breast tumor cell lines (HCC202, HCC1942 and AU565) that highly expressing HER1 and HER2, BMS-599626 treatment inhibited cell proliferation, while had no effect on A2780 cells that without HER1 or HER2 expression [1]. Treated OV202 cells with BMS-599626 significantly inhibited cell proliferation and enhanced cell apoptosis by inhibiting HER [2].
In mouse model with Sal2 tumor cells xenograft, oral administration of BMS-599626 inhibited Sal2 cells growth in a dose-dependent manner and significantly delayed tumor growth at the concentration of 60 mg/kg [1].
When tested with Sal2 cells expressing CD8-HER2 fusion protein, BMS-599626 treatment inhibited the receptor phosphorylation and MAPK phosphorylation with the IC50 value of 0.3 and 0.22 μM/L, respectively [1].
References:
[1].Wong, T.W., et al., Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res, 2006. 12(20 Pt 1): p. 6186-93.
[2].Haluska, P., et al., HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol Cancer Ther, 2008. 7(9): p. 2589-98.

Chemical Properties

StorageStore at -20°C
M.Wt567.01
Cas No.873837-23-1
FormulaC27H28ClFN8O3
SynonymsAC480;BMS-599626 HCl;BMS599626;BMS 599626;AC-480
SolubilitySoluble 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;hydrochloride
SDFDownload SDF
Canonical SMILESCC1=C2C(=NC=NN2C=C1NC(=O)OCC3COCCN3)NC4=CC5=C(C=C4)N(N=C5)CC6=CC(=CC=C6)F.Cl
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Quality Control

Quality Control & MSDS

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Chemical structure

BMS-599626 Hydrochloride