货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S85429-5mg	≥99%	￥890.00 S85429-5mg ￥890.00 3-5天	0 货期：3-5天	-	-	-	-
S85429-10mg	≥99%	￥1480.00 S85429-10mg ￥1480.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S85429-5mg

≥99%

￥890.00

货期：3-5天

S85429-10mg

≥99%

￥1480.00

货期：3-5天

产品描述：

AV-412 (MP412) 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);EGFRL858R:0.5 nM (IC50);EGFRT790M:0.79 nM (IC50);EGFRL858R/T790M:2.3 nM (IC50);ErbB2:19 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	1.175 ml	5.873 ml	11.745 ml
5 mM	0.235 ml	1.175 ml	2.349 ml
10 mM	0.117 ml	0.587 ml	1.175 ml
50 mM	0.023 ml	0.117 ml	0.235 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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