BMS 599626 dihydrochloride ((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)

name

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

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.

MW

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

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.

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.