您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > AV-412 free base
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
AV-412 free base
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AV-412 free base图片
CAS NO:451492-95-8
规格:98%
分子量:507
包装与价格:
包装价格(元)
200mg电议
500mg电议
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
AV-412 free base (MP-412 free base) 是 EGFR 抑制剂,抑制EGFR,EGFRL858R,EGFRT790M,EGFRL858R/T790M 和 ErbB2的 IC50 值分别为0.75,0.5,0.79,2.3,19 nM。
CAS:451492-95-8
分子式:C27H28ClFN6O
分子量:507
纯度:98%
存储:Store at -20°C

Background:

AV-412 free base (MP-412 free base) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. EGFR|0.75 nM (IC50)|ErbB2|19 nM (IC50)|EGFRL858R|0.51 nM (IC50)|EGFRL858R/T790M|2.3 nM (IC50)|EGFRT790M|0.79 nM (IC50)


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[1].


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[1].


[1]. Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptorand ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.