AG1024

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

CAS号

65678-07-1

分子式

C14H13BrN2O

主要靶点

Apoptosis|IGF-1R

仅限科研使用

Cat No : CM04705

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Synonyms

Tyrphostin|AGS 200|Tyrphostin AG 1024



产品信息

AG-1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).

CAS号 65678-07-1
分子式 C14H13BrN2O
主要靶点 Apoptosis|IGF-1R
主要通路 蛋白酪氨酸激酶|凋亡
分子量 305.17
纯度 98.00%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 Tyrphostin|AGS 200|Tyrphostin AG 1024

靶点活性

IGF-1R:7 μM|Insulin Receptor:57 μM

体内活性

AG-1024能够阻断IGF-1受体(IC50=7 μM)和IR(IC50=57 μM)自磷酸化。在MCF-7 细胞中,AG-1024 (10 μM) 能够能够下调磷酸化Akt1和bcl-2,上调Bax,p53和p21,从而抑制细胞增殖。

体外活性

在携带有Ba / F3-p210异种移植物小鼠中,AG-1024(30 μg)施用10天能够显著抑制肿瘤生长.

溶解度

H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:57 mg/mL (186.78 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

细胞实验

Cells are exposed to AG-1024 for 24, 48 or 72 hours. For the determination of proliferation, cells are harvested and counted with trypan blue dye exclusion. Apoptosis is evaluated by dual staining of MCF-7 with fluoresceine anti-digoxigenin and propidium iodide. Briefly, fixed cells are washed with PBS, suspended in TdT buffer with TdT enzyme and Dig-dUTP for 60 minutes, and suspended in FITC blocking solution with anti-Dig-Fluorescein for 30 minutes at room temperature and kept in a dark place. Cells are then rinsed in buffer and resuspended in propidium iodide/RNase A solution for 30 minutes then analyzed by flow cytometry. For the assessment of phospho-Akt1, Bax, p53, bcl-2 and p21, cells are lysed and analyzed by western blot.(Only for Reference)

参考文献

1.Párrizas M, et al. Endocrinology. 1997 Apr;138(4):1427-33.
2.Wen B, et al. Br J Cancer, 2001, 85(12), 22017-2021.
3.von Willebrand M, et al. Cancer Res, 2003, 63(6), 1420-1429.
4.Deutsch E, et al. Br J Cancer, 2004, 91(9), 1735-1741.

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