BMS 599626 dihydrochloride

Cat. No. 5022

BMS 599626 dihydrochloride C27H27FN8O3.2HCl

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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

Biological Activity

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

M.Wt:
603.48
Formula:
C27H27FN8O3.2HCl
Solubility:
Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO
Purity:
>98 %
Storage:
Store at -20°C

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

Gavai 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 6527. PMID: 19821562.

Wong et al (2006) Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin.Cancer Res. 12 6186. PMID: 17062696.

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