NVP-ADW742

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Chemical Structure| 475488-23-4 同义名 : ADW742; GSK 552602A; ADW
CAS号 : 475488-23-4
货号 : A507729
分子式 : C28H31N5O
纯度 : 98%
分子量 : 453.58
MDL号 : MFCD16038913
存储条件：

Pure form Keep in dark place, sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(39.68 mM)，配合低频超声助溶，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
生物活性
靶点

  • IGF-1R

    IGF-1R, IC50:0.17 μM
描述 NVP-ADW742 is an selective IGF-1R inhibitor with IC50 of 0.17 μM, > 16-fold more potent against IGF-1R than InsR and shows little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
MiaPaCa2 cells Function assay Inhibition IGF1R phosphorylation in human MiaPaCa2 cells, IC50=0.323 μM 17689078
Sf21 cells Function assay Inhibition of human IGF1R expressed in Sf21 cells by time-resolved fluorescence assay, IC50=0.078 μM 17689078
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.20mL

0.44mL

0.22mL

11.02mL

2.20mL

1.10mL

22.05mL

4.41mL

2.20mL
参考文献

[1]Mitsiades CS, Mitsiades NS, et al. Inhibition of the insulin-like growth factor receptor-1 tyrosine kinase activity as a therapeutic strategy for multiple myeloma, other hematologic malignancies, and solid tumors. Cancer Cell. 2004 Mar;5(3):221-30.

[2]Warshamana-Greene GS, Litz J, et al. The insulin-like growth factor-I (IGF-I) receptor kinase inhibitor NVP-ADW742, in combination with STI571, delineates a spectrum of dependence of small cell lung cancer on IGF-I and stem cell factor signaling. Mol Cancer Ther. 2004 May;3(5):527-35.