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Submit ReviewBMS 599626 dihydrochloride is a 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.
分子量 | 603.48 |
公式 | C27H27FN8O3.2HCl |
储存 | Store at -20°C |
纯度 | ≥98% (HPLC) |
CAS Number | 1781932-33-9 |
PubChem ID | 90488998 |
InChI Key | SKHKFWSXLCGMNF-IKXQUJFKSA-N |
Smiles | FC1=CC(CN2N=CC3=C2C=CC(NC4=NC=NN5C4=C(C)C(NC(OC[C@@H]6COCCN6)=O)=C5)=C3)=CC=C1.Cl.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
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 efficaciou J.Med.Chem. 52 6527 PMID: 19821562
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