公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! 抑制剂描述: 产品名称:AV-412 free base 产品别名:见爱必信官网 英文别名:AV-412 free base 靶点:EGFR CAS:451492-95-8 纯度:98% 外观:见爱必信官网 保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. 描述: AV-412(MP-412)是EGFR和ErbB2的双重抑制剂,能抑制突变型EGFR(L858R和T790M,IC50分别为0.51 nM和0.79 nM),还能抑制EGFR和ErbB2的自磷酸化,IC50分别为43和282 nM。 溶解性:DMSO : 50 mg/mL (98.62 mM; Need ultrasonic) 体外研究: AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC50 of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. 体内研究:In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. 产品信息订购:
产品更多信息请进入爱必信(absin)商城查看》》》
absin,您身边的科研百宝箱 专业提供试剂、耗材、仪器,在线订购,7*24h全国发货,方便快捷! |