2. Protein Tyrosine Kinase/RTK
  3. Bcr-Abl
  4. AG957

AG957  (Synonyms: Tyrphostin AG957; NSC 654705)

目录号: HY-117718 纯度: 99.30%
COA 产品使用指南

摩尔计算器

AG957 (Tyrphostin AG957;NSC 654705) 是一种酪氨酸激酶抑制剂，具有抗 BCR/ABL 酪氨酸激酶活性。AG957抑制 p210bcr/abl 酶活性，IC50 为 2.9 μM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

AG957 Chemical Structure

AG957 Chemical Structure

CAS No. : 140674-76-6

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
5 mg ￥1450
In-stock
10 mg ￥2320
In-stock
25 mg ￥4880
In-stock
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

AG957 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AG957 (Tyrphostin AG957;NSC 654705) is a tyrosine kinase inhibitor with anti-BCR/ABL tyrosine kinase activity[1][2]. AG957 is a bcr/abl kinase inhibitor with an IC50 of 2.9 μM for p210bcr/abl autokinase activity[3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
23.2 μM
Compound: 4d
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 34284106]
Caco-2 IC50
15.1 μM
Compound: 4d
Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human Caco-2 cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 34284106]
Jurkat IC50
13.1 μM
Compound: 4d
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
Cytotoxicity against human Jurkat cells assessed as cell growth inhibition measured after 72 hrs by CCK8 assay
[PMID: 34284106]
体外研究
(In Vitro)

AG957 inhibit p210bcr-abl tyrosine kinase activity. AG957 inhibits DNA synthesis as early as 2 h (60% inhibition at 20 microM). AG957 inhibits p210bcr-abl tyrosine phosphorylation in living cells by 1 h without an inhibition of total protein phosphorylation[1]. Tyrphostin AG957, a protein tyrosine kinase (PTK) inhibitor which has activity against the p210BCR/ABL kinase, on beta1 integrin function in CML progenitors[2].
AG957 (0.1-100 μM ) pretreatment results in significant inhibition of proliferation of chronic myelogenous leukemia (CML) colony-forming cells (CFC) CML CFC[2].
AG957 (25 μM) partially inhibits phosphorylation of several proteins that are BCR/ABL PTK substrates and are involved in normal integrin signaling in BCR/ABL expressing cells[2].

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

AG957 相关抗体:

Cell Proliferation Assay[2]

Cell Line: CML and CFC
Concentration: 0, 0.1, 1, 10, 100 μM
Incubation Time: Pretreatment for 1 hour
Result: A significant dose-dependent inhibition of CML CFC growth was seen following preincubation with AG957.

Western Blot Analysis[2]

Cell Line: K562 and BCR/ABL-tranfected M07e cells (MBA-4)
Concentration: 25 μM
Incubation Time: 24 hours
Result: Partially inhibited tyrosine phosphorylation of p210BCR/ABL, the focal adhesion protein paxillin, the p85 regulatory subunit of the PI3K and the adapter protein cbl in K562 cells.
Inhibited phosphorylation of these proteins as well as the adapter protein crkl in MBA4 cells.
体内研究
(In Vivo)

AG957 (10 mg/kg; intratracheally 1 h before intratracheal LPS challenge) blocks c-Abl activity in the lung of mice[4].

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

Animal Model: C57BL/6J mice[4]
Dosage: 10 mg/kg
Administration: Intratracheally 1 h before intratracheal LPS challenge
Result: LPS induced significant phosphorylation of paxillin at Y31 and Y118. Inhibition of c-Abl by AG957 attenuated LPS-induced phosphorylation of paxillin at both sites.
LPS induced significant phosphorylation of VE-cadherin in DMSO-treated mice, which was attenuated in AG957-treated mice.
分子量

273.28

Formula

C15H15NO4
CAS 号
性状

固体

颜色

Off-white to light brown

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (365.93 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6593 mL 18.2963 mL 36.5925 mL
5 mM 0.7319 mL 3.6593 mL 7.3185 mL
查看完整储备液配制表

* 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。-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。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

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

  • 方案 一

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

    Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (9.15 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献

AG957 相关分类

完整储备液配制表

* 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。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6593 mL 18.2963 mL 36.5925 mL 91.4813 mL
5 mM 0.7319 mL 3.6593 mL 7.3185 mL 18.2963 mL
10 mM 0.3659 mL 1.8296 mL 3.6593 mL 9.1481 mL
15 mM 0.2440 mL 1.2198 mL 2.4395 mL 6.0988 mL
20 mM 0.1830 mL 0.9148 mL 1.8296 mL 4.5741 mL
25 mM 0.1464 mL 0.7319 mL 1.4637 mL 3.6593 mL
30 mM 0.1220 mL 0.6099 mL 1.2198 mL 3.0494 mL
40 mM 0.0915 mL 0.4574 mL 0.9148 mL 2.2870 mL
50 mM 0.0732 mL 0.3659 mL 0.7319 mL 1.8296 mL
60 mM 0.0610 mL 0.3049 mL 0.6099 mL 1.5247 mL
80 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1435 mL
100 mM 0.0366 mL 0.1830 mL 0.3659 mL 0.9148 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AG957140674-76-6Tyrphostin AG957 NSC 654705AG 957AG-957Tyrphostin AG 957Tyrphostin AG-957NSC654705NSC 654705NSC-654705Bcr-AblChronicmyelogenousleukemiaintegrinstyrosinekinaseBCR/ABLhematopoiesispaxillinc-AbllipopolysaccharidecytoskeletonInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
AG957
目录号：
HY-117718
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z