货号 | 5022/10 |
别名 | (3S)-3-Morpholinylmethyl-[4-[[1-[(3 |
供应商 | Tocris |
生物活性 | 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. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >98 % |
计算分子量 | 603.48 |
分子式 | C27H27FN8O3< |
可溶性/溶解性 | Soluble to 5 mM in water with gentle warming and to 100 mM in DMSO |
参考文献 | Gavaiet 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. Wonget 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. |