AG1024 (Synonyms:Tyrphostin AG 1024)
目录号 : KM4411 CAS No. : 65678-07-1 纯度 : 98%

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。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

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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.

体外研究

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

Cell Proliferation Assay

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

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

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

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

Animal Model: Female nude mice (6-8 weeks old)
Dosage: 30 μg
Administration: IP; per day; for 2 weeks
Result: Significantly delayed the tumour growth.
分子式
C14H13BrN2O
分子量
305.17
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。

科研文献
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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