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AG1024

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Chemical Structure| 65678-07-1 同义名 : Tyrphostin AG 1024;AGS 200;AG 1024. Tyrphostin.;Tyrphostin
CAS号 : 65678-07-1
货号 : A114134
分子式 : C14H13BrN2O
纯度 : 98%
分子量 : 305.17
MDL号 : MFCD02179365
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(163.84 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • IGF-1R

    IGF-1R, IC50:7 μM

  • Insulin Receptor

    Insulin Receptor, IC50:57 μM
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.28mL

0.66mL

0.33mL

16.38mL

3.28mL

1.64mL

32.77mL

6.55mL

3.28mL
参考文献

[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