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。
| 生物活性 | AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selectiveIGF-1Rinhibitor with anIC50of 7 μM. AG1024 inhibits phosphorylation ofIR(IC50=57 μM). AG1024 inducesapoptosisand 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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(163.84 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 *以上所有助溶剂都可在本网站选购。
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