Molecular Formula | C27H31N7O2 |
Molar Mass | 485.58 |
Density | 1.267±0.06 g/cm3(Predicted) |
Melting Point | 158 - 160°C |
Solubility | DMSO: ≥ 28 mg/mL |
Appearance | Solid |
Color | Off-White |
pKa | 12.68±0.70(Predicted) |
Storage Condition | Refrigerator |
In vitro study | AZ5104 showed good efficacy against ex19del (2 nM in PC-9),T790M (2 nM in H1975), and wild-type EGFR (33 nM in LOVO) cell lines. AZ5104 caused the inhibition of cell activity, and the IC50 of H1975 (T790M/L858R),PC-9 (ex19del),Calu 3 (WT), and NCI-H2073 (WT) were 3.3 nM, respectively, 2.6 nM,80 nM, and 53 nM. |
In vivo study | AZ5104 (5 mg/kg/d, p.o.) induced significant and sustained tumor regression in C/L858R and C/L T mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.059 ml | 10.297 ml | 20.594 ml |
5 mM | 0.412 ml | 2.059 ml | 4.119 ml |
10 mM | 0.206 ml | 1.03 ml | 2.059 ml |
5 mM | 0.041 ml | 0.206 ml | 0.412 ml |