Catalog Number: 5022
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.
Background References
  1. 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
  2. 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

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