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CAS No.: 65678-07-1

AG1024 Catalog No. CSN13710

Synonyms: Tyrphostin AG 1024;Tyrphostin;AGS-200

AG1024 inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Insulin Receptor

IC50:57μM IGF-1R

IC50:7μM
描述IGF-1R (insulin-like growth factor-1 receptor) plays a key role in transformation, growth and survival of malignant cells, and has been considered as a general and promising target for cancer treatment. AG1024 is a selective IGF-1R inhibitor with IC50 value of 7μM for inhibition of IGF-1R autophosphorylation in NIH-3T3 cells, also inhibits IR with IC50 of 57μM. AG1024 inhibited the IGF-1-induced MAPK signal-regulated kinase pathway in metastatic melanoma cells (501 mel) treated with 4μM AG1024 for 30min. And a longer treatment of AG1024 led to a restore of pRb tumor suppressive function as the reduction in the phosphorylated forms of pRb, p107 and p130 due to proteasomal and nonproteasomal degradation, and the formation of growth suppressive DNA binding complexes consisting of pRb and E2F1 or E2F3 could be observed^[2].
动物研究
剂量
Nude Mice: 1.5 mg/kg^[3] (i.p.); 100 mg/kg^[4] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Nude Mice: 1.5 mg/kg^[3] (i.p.); 100 mg/kg^[4] (p.o.)
给药途径	i.p., p.o.

[1] P¨¢rrizas M, Gazit A, et al. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.
[2] von Willebrand M, Zacksenhaus E, et al. The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells. Cancer Res. 2003 Mar 15;63(6):1420-9

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 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

技术信息

CAS号

65678-07-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C14H13BrN2O

运输

蓝冰

分子量

305.17

别名

Tyrphostin AG 1024;Tyrphostin;AGS-200

溶解度

DMSO	61.0 mg/mL (199.9 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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靶点	Description	IC50
Insulin Receptor		IC50:57μM
IGF-1R		IC50:7μM

AG1024 Catalog No. CSN13710

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