1-[[4-[(4-氟-2-甲基-1H-吲哚-5-基)氧基]-5-甲基吡咯并[2,1-f][1,2,4]三嗪-6-基]氧基]-2-丙醇

溶解度:Soluble in DMSO

储存条件:-20C 2 years

生物活性

BIBW-2992 is a potent oral, irreversible combined EGFR/HER2 inhibitor both in vitro and in vivo. The potency of BIBW-2992 on the EGFR and HER2 kinases revealed IC50 values of 0.5 nM and 14 nM, respectively. BIBW-2992 is highly selective for these kinases

参考文献

1. BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models. Li, D., Ambrogio, L., Shimamura, T., Kubo, S., Takahashi, M., Chirieac, L.R., Padera, R.F., (...), Wong, K.-K.. 2008 Oncogene 27 (34), pp. 4702-4711(cant find full text or PDF)

2. Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer. Riely, G.J. 2008 Journal of Thoracic Oncology 3 (6 SUPPL 2), pp. S146-S149

3. Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). Reid A, Vidal L, Shaw H, de Bono J. Eur J Cancer. 2007 Feb;43(3):481-9. Epub 2007 Jan 8. Review.