Molecular Formula | C22H23ClFN5O3 |
Molar Mass | 459.9 |
Density | 1.358±0.06 g/cm3(Predicted) |
Boling Point | 571.4±50.0 °C(Predicted) |
Solubility | 10 mM in DMSO |
pKa | 6.71±0.40(Predicted) |
Storage Condition | -20℃ |
In vitro study | In H3255 (L858R) cells, AZD3759 inhibits EGFR phosphorylation with an IC50 of 7.2 nM. AZD3759 showed an inhibitory effect on the proliferation of PC-9 and H3255 cells derived from pEGFR pathway and EGFR mutant gene, with IC50 of 7.7 nM and 7 nM, respectively, and had no activity on the proliferation of H838 cells. |
In vivo study | AZD3759 showed good oral activity in dogs and was able to penetrate extensively into the monkey brain. In the brain metastatic PC-9 (Exon19Del) model, AZD3759 (15 mg/kg) caused a significant dose-dependent antitumor effect. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.174 ml | 10.872 ml | 21.744 ml |
5 mM | 0.435 ml | 2.174 ml | 4.349 ml |
10 mM | 0.217 ml | 1.087 ml | 2.174 ml |
5 mM | 0.043 ml | 0.217 ml | 0.435 ml |