AG-1024
(Synonyms: Tyrphostin AG 1024) 目录号 : GC13697
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值为7µM。AG-1024能够抑制胰岛素受体（IR）的磷酸化，IC50值为57µM。
Cas No.:65678-07-1
Sample solution is provided at 25 µL, 10mM.
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AG-1024 is a reversible, competitive and selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 value of 7µM[1]. AG-1024 can inhibit the phosphorylation of insulin receptor (IR) with an IC50 value of 57µM[2]. AG-1024 can induce cell apoptosis and has anti-cancer activity[3].
In vitro, AG-1024 (5µM) treatment of acquired sorafenib-resistant cell lines (SNU-sora-5 and SK-sora-5 cells) for 72h significantly increased the cytotoxicity of sorafenib, activated the intracellular mTOR/P21 signaling pathway, and enhanced the cell G1/S arrest[4]. AG-1024 (10μM) treatment of PC3 and DU145 cells inhibited cell proliferation and induced cell G2/M phase arrest[5].
In vivo, oral administration of AG-1024 (20mg/kg) to diabetic nephropathy model rats for 8 weeks alleviated metabolic disorders, improved renal function, reduced renal inflammation, and reduced renal fibrosis formation[6].
References:
[1] Xue M, Cao X, Zhong Y, et al. Insulin-like growth factor-1 receptor (IGF-1R) kinase inhibitors in cancer therapy: advances and perspectives[J]. Current pharmaceutical design, 2012, 18(20): 2901-2913.
[2] Talior-Volodarsky I, Mahou R, Zhang D, et al. The role of insulin growth factor-1 on the vascular regenerative effect of MAA coated disks and macrophage-endothelial cell crosstalk[J]. Biomaterials, 2017, 144: 199-210.
[3] Cheng H Y, Ko F H. Studying the enhancement of programmed cell death by combined AG1024 and paclitaxel in a model of chronic myelogenous leukemia[J]. Life sciences, 2014, 102(2): 118-126.
[4] Zhou W, Lou W, Chen J, et al. AG-1024 Sensitizes Sorafenib-Resistant Hepatocellular Carcinoma Cells to Sorafenib via Enhancing G1/S Arrest[J]. OncoTargets and therapy, 2021: 1049-1059.
[5] Tang Q, Ma J, Sun J, et al. Genistein and AG1024 synergistically increase the radiosensitivity of prostate cancer cells[J]. Oncology Reports, 2018, 40(2): 579-588.
[6] Liu J, Zhang Y, Liu M, et al. AG1024, an IGF-1 receptor inhibitor, ameliorates renal injury in rats with diabetic nephropathy via the SOCS/JAK2/STAT pathway[J]. Open Medicine, 2023, 18(1): 20230683.
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值为7µM[1]。AG-1024能够抑制胰岛素受体（IR）的磷酸化，IC50值为57µM[2]。AG-1024能够诱导细胞凋亡，具有抗癌活性[3]。
在体外，AG-1024（5µM）处理获得性索拉非尼耐药细胞系（SNU-sora-5和SK-sora-5细胞）72h，显著提高了索拉非尼对细胞的毒性，激活了细胞内mTOR/P21信号通路，增强了细胞G1/S阻滞[4]。AG-1024（10μM）处理PC3和DU145细胞，抑制了细胞增殖，诱导了细胞G2/M期阻滞[5]。
在体内，AG-1024（20mg/kg）通过口服治疗糖尿病肾病模型大鼠8周，减轻了代谢紊乱，改善了大鼠的肾功能，减轻了肾脏炎症，减少了肾纤维化形成[6]。
| Cell experiment [1]: | |
Cell lines | SNU-sora-5、SK-sora-5 cells |
Preparation Method | SNU-sora-5 and SK-sora-5 were exposed to a series of concentrations of sorafenib with or without 5μM AG-1024 for 72h. The IC50 values of Sorafenib were determined. |
Reaction Conditions | 5µM; 72h |
Applications | AG-1024 dramatically improve the cytotoxicity of sorafenib in acquired sorafenib-resistant cells. |
| Animal experiment [2]: | |
Animal models | Wistar rats |
Preparation Method | Rats were randomly assigned into the control, the DN, the DN+AG-1024, and the DN+metformin groups. Each group had 15 rats. The overnight-fasted rats were intraperitoneally injected with 2% pentobarbital sodium (40mg/kg) followed by the removal of the right kidneys. The controls were injected once with citrate buffer and 0.5mL saline daily for 12 weeks. After 2 weeks, the rats in the DN groups received a single intraperitoneal injection of freshly prepared streptozotocin (STZ; 50mg/kg). After 4 weeks of cultivation, the diabetic rats in the DN group received 0.5mL saline daily, those in the DN+AG-1024 group were administered with AG-1024 (20mg/kg/day, p.o.), and those in the DN+metformin group were given with metformin (200mg/kg/day) by gavage for 8 weeks. |
Dosage form | 20mg/kg for 8 weeks; p.o. |
Applications | AG-1024 can reduce metabolic disorders in the experimental rat model of diabetic nephropathy. AG-1024 can improve renal function, reduce renal inflammation, and reduce renal fibrosis formation in diabetic rats. |
References: | |
| Cas No. | 65678-07-1 | SDF | |
| 别名 | Tyrphostin AG 1024 | ||
| 化学名 | 2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile | ||
| Canonical SMILES | CC(C)(C)C1=C(C(=CC(=C1)C=C(C#N)C#N)Br)O | ||
| 分子式 | C14H13BrN2O | 分子量 | 305.17 |
| 溶解度 | ≥ 15.25mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 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 | g | |
每只动物给药体积 | ul | |
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GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 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，
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 saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet