NVP-ADW742 是一种具有口服活性，选择性的IGF-1R酪氨酸激酶抑制剂，IC50为 0.17 μM。它抑制胰岛素受体，IC50为 2.8 μM，在肿瘤细胞中诱导多效性抗增殖/促凋亡。

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

CRT0044876 potently inhibits the AP endonuclease, 3'-phosphodiesterase and 3'-phosphatase activities of APE1, and exhibits the selectivity for the inhibition of exonuclease III family. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds with an accumulation of unrepaired AP sites. [1] CRT0044876, by inhibition of the BER pathway increases oxidative DNA damage temporally related to increased intracellular reactive oxygen species in an acidic tumor microenvironment, and thus results in cell cycle arrests and increased DNA double strand breaks, leading to cell death. [2]

475488-23-4

C28H31N5O

453.58

ADW;GSK 552602A;ADW742

H2O:<1 mgml
Ethanol:3 mg/mL (6.61 mM)
DMSO:10 mg/mL (22.04 mM),warmed
Powder: -20°C for 3 years
In solvent: -80°C for 2 years