货号	规格	价格	上海	北京	珠海	重庆	武汉
S85428-10mg	≥98%(HPLC)	￥396.00 S85428-10mg ￥396.00 现货	6 6	-	2	-	-
S85428-50mg	≥98%(HPLC)	￥659.00 S85428-50mg ￥659.00 现货	4 4	2	1	-	-
S85428-250mg	≥98%(HPLC)	￥1790.00 S85428-250mg ￥1790.00 现货	1 1	-	-	-	-

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产品描述：

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.

靶点：

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);EGFR

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

参考文献：

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.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.972 ml	9.862 ml	19.724 ml
5 mM	0.394 ml	1.972 ml	3.945 ml
10 mM	0.197 ml	0.986 ml	1.972 ml
50 mM	0.039 ml	0.197 ml	0.394 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

AV 412,EGFR，ErbB2和Abl受体酪氨酸激酶的有效抑制剂

AV-412 (free base)

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)