Molecular Formula | C24H25N5O4 |
Molar Mass | 447.49 |
Solubility | DMSO: ≥ 41 mg/mL |
Storage Condition | -20℃ |
In vitro study | AZD2932 effectively inhibits the activities of VEGFR-2 (IC50, 8 nM), PDGFRβ (IC50,4 nM), Flt-3 (IC50, 7 nM), and c-Kit (IC50, 9 nM). AZD2932 inhibits both PDGFRα and PDGFRβ phosphorylation with a correlation close to 1:1. AZD2932 does not inhibit the various cytochrome P450 isoforms with the worst IC50 being against 2C9 (8.0 μM). AZD2932 has no activity against hERG (IC50, 137 μM). |
In vivo study | In C6 rat glial tumor model, AZD2932 (p.o., b.i.d.) results in significant TGI of 64% for both 50 and 12.5 mg/kg doses. Growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. (p.o.) and LoVo tumors by 67% at 50 mg/kg b.i.d (p.o.). AZD2932 (3–50 mg/kg, p.o.) causes 60–80% inhibition of both p-VEGFR-2 and p-PDGFRβ. Single bolus oral doses of AZD2932 results in dose-related inhibition of PDGFRa phosphorylation 6 h after dosing. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.235 ml | 11.174 ml | 22.347 ml |
5 mM | 0.447 ml | 2.235 ml | 4.469 ml |
10 mM | 0.223 ml | 1.117 ml | 2.235 ml |
5 mM | 0.045 ml | 0.223 ml | 0.447 ml |