Avitinib - CAS:1557267-42-1

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Avitinib (Synonyms:艾维替尼; Abivertinib; AC0010)

目录号 : KCM11678 CAS No. : 1557267-42-1 纯度 : ≥98%

Data Sheet 产品使用指南

Avitinib is a pyrrolopyrimidine-based, irreversible inhibitor of the epidermal growth factor receptor (EGFR). It is selective for EGFR-active and T790M mutations, exhibiting a 298-fold increase in potency compared with wild-type EGFR. In a xenograft model, oral administration of 500 mg/kg avitinib was shown to result in complete remission of tumors with EGFR-active and T790M mutations.

规格	价格	是否有货
10 mM * 1 mL in DMSO	¥675.00	In-stock
5mg	¥630.00	In-stock
10mg	¥1080.00	In-stock
25mg	¥1980.00	In-stock

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生物活性

Avitinib is a third-generation, irreversible and orally active selective EGFR inhibitor, with IC₅₀ values of 0.18 nM, 0.18 nM, 7.68 nM and against EGFR L858R, EGFR T790M and wild-type EGFR. Avitinib is also a BTK inhibitor that induces apoptosis and inhibits phosphorylation of BTK in mantle cell lymphoma. Avitinib shows anticancer effects.

IC₅₀&Target

EGFR L858R EGFR^T790M

0.18 nM (IC₅₀) 0.18 nM (IC₅₀)

体外研究

Avitinib (AC0010; 0.13 nM-2 μM; 2 h) selectively inhibits mutant EGFR phosphorylation in NCI-H1975 and NIH/3T3_TC32T8 cells, with IC₅₀ values of 7.3 and 2.8 nM, respectively. It is approximately 115 times and 298 times more sensitive to inhibition than wild-type EGFR in A431. Avitinib effectively inhibits EGFR-Tyr1068 phosphorylation in NCI-H1975 cells, and the selectivity of NCI-H1975 cells is 65 times higher than that of A431 cells. In addition to inhibiting the phosphorylation of EGFR-Tyr1068, Avitinib also inhibits the phosphorylation of downstream targets Akt and ERK1/2 in NCI-H1975 and HCC827 cells .

Western Blot Analysis

Cell Line:	NCI-H1975, HCC827, A431 cells
Concentration:	0.13 nM, 0.64 nM, 3.2 nM, 16 nM, 80 nM, 0.4 μM, 2 μM
Incubation Time:	2 hour
Result:	Selectively inhibits mutant EGFR phosphorylation with IC50 values of 7.3 and 2.8 nM in NCI-H1975 and NIH/3T3_TC32T8 cells.

体内研究

Avitinib (AC0010; 12.5-500 mg/kg; oral; Once a day; Long term inhibition of EGFR mutant tumor growth in a xenograft model lasting for 14 days, but not inhibition of wild-type EGFR tumor growth .

Animal Model:

Nu/Nu nude mice (Six- to 8-week-old) injected with NCI-H1975 and A431 cells

Dosage:

12.5, 50, and 500 mg/kg

Administration:

Orally administration; once daily; for 14 days

Result:

Inhibited EGFR-mutant tumor growth but not wild-type EGFR tumor growth.

分子式

C₂₆H₂₆FN₇O₂

分子量

487.53

CAS号

1557267-42-1

中文名称

艾维替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

2-8°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (170.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0512 mL	10.2558 mL	20.5116 mL
5 mM	0.4102 mL	2.0512 mL	4.1023 mL
10 mM	0.2051 mL	1.0256 mL	2.0512 mL

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂：10% DMSO → 40% PEG300 → 5% Tween-80 → 45% saline

Solubility: ≥ 3.57 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 3.57 mg/mL (7.32 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 35.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂：10% DMSO → 90% corn oil

Solubility: ≥ 3.57 mg/mL (7.32 mM); Clear solution

此方案可获得 ≥ 3.57 mg/mL (7.32 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 35.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

纯度： ≥98%

Data Sheet

产品使用指南

Xu X, Mao L, Xu W, 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;15(11):2586-2597.

Yan X, Zhou Y, Huang S, et al. Promising efficacy of novel BTK inhibitor AC0010 in mantle cell lymphoma. J Cancer Res Clin Oncol. 2018;144(4):697-706.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量

浓度

体积

分子量*

重置计算

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

重置计算

动物实验计算换算器

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

每只动物给药体积

动物数量

只

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，请联系客服为您提供正确的澄清溶液配方）

% DMSO

% Tween 80

% ddH₂O

% DMSO

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系客服）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

配置后的溶液总体积：

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 0 篇科研文献

The molarity calculator equation

The dilution calculator equation

动物实验计算换算器