AG1024(Synonyms: Tyrphostin AG 1024)

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AG1024 (Synonyms: Tyrphostin AG 1024) 纯度: 98.86%

AG1024 (Tyrphostin AG 1024) 是一种可逆的，竞争性和选择性的胰岛素样生长因子-1 受体 (IGF-1R) 抑制剂，IC50 为 7 μM。AG1024 抑制胰岛素受体 (IR) 的磷酸化 (IC50=57 μM)。AG1024 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。

AG1024(Synonyms: Tyrphostin AG 1024)

AG1024 Chemical Structure

CAS No. : 65678-07-1

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥660 In-stock
5 mg ￥600 In-stock
10 mg ￥1100 In-stock
50 mg ￥3500 In-stock
100 mg ￥6000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

AG1024 相关产品

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生物活性

AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity[1][2].

IC50 & Target

IC50: 7 μM (IGF1R) and 57 μM (IR)[1][2]
体外研究
(In Vitro)

AG1024 (Tyrphostin AG 1024; 2-10 μM; 1-5 days) shows a dose-dependent inhibition of cell proliferation[1].
AG1024 (1-5 μM; 1-3 days) induces UT7-9 and Baf3-p210 cells apoptosis[1].
AG1024 (2 μM; 6, 12 hours) downregulates phospho-Akt, Bcr-Abl and upregulates DNA-PKcs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: UT7-9 and Baf3-p210 cells
Concentration: 2, 5, 10 μM
Incubation Time: 1, 3, 5 days
Result: Showed a dose-dependent inhibition of cell proliferation.

Apoptosis Analysis[1]

Cell Line: UT7-9 and Baf3-p210 cells
Concentration: 1, 3, 5 μM
Incubation Time: 1, 2, 3 days
Result: Induced apoptosis.

Western Blot Analysis[1]

Cell Line: UT7-9 and Ba/F3-p210 cells
Concentration: 2 μM
Incubation Time: 6, 12 hours
Result: Downregulated phospho-Akt, Bcr-Abl and upregulated DNA-PKcs.

体内研究
(In Vivo)

AG1024 (Tyrphostin AG 1024; 30 μg; i.p.; per day; for 2 weeks) significantly delays the tumour growth[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female nude mice (6-8 weeks old)[1]
Dosage: 30 μg
Administration: IP; per day; for 2 weeks
Result: Significantly delayed the tumour growth.

分子量

305.17

Formula

C14H13BrN2O
CAS 号

65678-07-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (163.84 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2769 mL 16.3843 mL 32.7686 mL
5 mM 0.6554 mL 3.2769 mL 6.5537 mL
10 mM 0.3277 mL 1.6384 mL 3.2769 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。-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: ≥ 2.5 mg/mL (8.19 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.19 mM，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；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。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Párrizas M, et al. Specific inhibition of IGF-1R and IR tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.

    [2]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735-41.

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