BMS 599626 dihydrochloride
Chemical Name: (3S)-3-Morpholinylmethyl-[4-[[1-[(3-fluorophenyl)methyl]-1H-indazol-5-yl]amino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]-carbamate dihydrochloride
Purity: ≥98%
Biological Activity
BMS 599626 dihydrochloride is a potent and selective EGFR and ErbB2 inhibitor (IC50 values are 22 nM and 32 nM respectively). Also inhibits HER4 (IC50 = 190 nM). Inhibits EGFR and ErbB2 with 100-fold greater potency than MEK and Lck. Antiproliferative agent in vitro and anti-tumorigenic agent in vivo. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling.
Wong et al.
Clin.Cancer Res., 2006;12:6186 -
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 efficaciou
Gavai et al.
J.Med.Chem., 2009;52:6527
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