AV-412

CAS: 451493-31-5 货号: A654958 分子式: C41H44ClFN6O7S2 分子量: 851.41
有货
级别和纯度: 10mM in DMSO
储存条件
干燥,-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
A654958-1ml
期货 Stock Image
¥1,379.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

干燥,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


AV-412 (MP412) is an EGFR inhibitor with IC 50 s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR , EGFR L858R , EGFR T790M , EGFR L858R/T790M and ErbB2, respectively.

In Vitro

AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC 50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:EGFR 0.75 nM (IC 50 ) EGFR L858R 0.5 nM (IC 50 ) EGFR T790M 0.79 nM (IC 50 ) EGFR L858R/T790M 2.3 nM (IC 50 ) ErbB2 19 nM (IC 50 )

规格

规格或纯度
10mM in DMSO
英文名称
AV-412
生化机理
AV-412 (MP412) 是一种表皮生长因子受体抑制剂,对表皮生长因子受体、表皮生长因子受体 L858R、表皮生长因子受体 T790M、表皮生长因子受体 L858R/T790M 和 ErbB2 的 IC 50 s 分别为 0.75、0.5、0.79、2.3 和 19 nM。
储存条件
干燥,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.CC(C)(C#CC1=CC2=C(C=C1NC(=O)C=C)C(=NC=N2)NC3=CC(=C(C=C3)F)Cl)N4CCN(CC4)C
关联CAS
分子量
851.41

技术文档

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高级数据

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