Home>>Signaling Pathways>> Tyrosine Kinase>> EGFR>>Avitinib maleate

Avitinib maleate Sale

(Synonyms: 艾维替尼马来酸盐; Abivertinib maleate; AC0010 maleate) 目录号 : GC19044

A selective inhibitor of mutant EGFR

Avitinib maleate Chemical Structure

Cas No.:1557268-88-8

规格 价格 库存 购买数量
5mg
¥483.00
现货
10mg
¥819.00
现货
50mg
¥3,077.00
现货
100mg
¥4,914.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Cell experiment:

Cell proliferation is assayed by a cell viability reagent, WST-1. Cells are seeded at optimal density onto 96-well plates and incubated for 24 hours, followed by avitinib treatment for 72 hours. Cell viability is then assayed by incubating cells with WST-1 reagent for 2-3 hrs[1].

Animal experiment:

Rats: To assess the potential skin toxicity of avitinib, a rat model is used. Rats are administrated daily with avitinib at 300 mg/kg for 4 weeks, and in control groups gefitinib at 50mg/kg or vehicle control (0.5% MC) is administrated[1]. Mice: NCI-H1975 tumor bearing mice are orally treated with a vehicle control (0.5% MC), avitinib at dose levels of 12.5 mg/kg and 50 mg/kg for 17 days when TV value in vehicle control group reached approximately 2000 mm3 . After 17-day dosing, animals in the vehicle control group are sacrificed, whereas animals in avitinib groups are continually daily administrated with increased dose at 500 mg/kg till the test mice cannot tolerate the treatment. Mouse body weight and TV are measured twice per week. TV is then used for the calculation of tumor inhibitory rate and tumor regression rate[1].

References:

[1]. Xu X, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597.

产品描述

Avitinib maleate is a pyrrolopyrimidine-based irreversible epidermal growth factor receptor (EGFR) inhibitor with an IC50 of 7.68 nM.

Avitinib is structurally distinct from previously reported pyrimidine-based irreversible EGFR inhibitors such as osimertinib and rociletinib. Avitinib is designed specifically to inhibit EGFR active mutations and the T790M acquired resistant mutation, while sparing wild type EGFR. Avitinib selectively inhibits EGFR active and T790M mutations with up to 298-fold increase in potency compared to wild-type EGFR. Avitinib exhibits potent inhibitory activity with IC50 value of 0.18 nM against EGFR L858R/T790M double mutations, nearly 43-fold greater potency over wild-type EGFR (IC50=7.68 nM). Avitinib selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 nM and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells, about 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431[1].

Oral administration of avitinib at daily dose of 500 mg/kg results in complete remission of tumors with EGFR active and T790M mutations for over 143 days with no weight loss. Three major metabolites of avitinib are tested and show no wild-type EGFR inhibition and off-target effects such as inhibition of IGF-1R. Avitinib is safe in non-small cell lung cancer (NSCLC) patients at the dose range between 50 mg and 550 mg once per day and no hyperglycemia and other severe adverse effects are detected such as grade 3 QT prolongation[1].

References:
[1]. Xu X, et al. AC0010, an Irreversible EGFR Inhibitor Selectively Targeting Mutated EGFR and Overcoming T790M-Induced Resistance in Animal Models and Lung Cancer Patients. Mol Cancer Ther. 2016 Nov;15(11):2586-2597.

Chemical Properties

Cas No. 1557268-88-8 SDF
别名 艾维替尼马来酸盐; Abivertinib maleate; AC0010 maleate
Canonical SMILES O=C(O)/C=C\C(O)=O.O=C(C=C)NC1=CC=CC(OC2=NC(NC3=CC(F)=C(N4CCN(C)CC4)C=C3)=NC5=C2C=CN5)=C1
分子式 C30H30FN7O6 分子量 603.6
溶解度 DMSO : ≥ 300 mg/mL (497.02 mM) 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 1.6567 mL 8.2836 mL 16.5673 mL
5 mM 0.3313 mL 1.6567 mL 3.3135 mL
10 mM 0.1657 mL 0.8284 mL 1.6567 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置