883986-34-3
883986-34-3 structure
- Name: AZD2932
- Chemical Name: Benzeneacetamide, 4-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[1-(1-methylethyl)-1H-pyrazol-4-yl]
- CAS Number: 883986-34-3
- Molecular Formula: C24H25N5O4
- Molecular Weight: 447.486
- Catalog: Biochemical Inhibitor Protein tyrosine kinase
- Create Date: 2017-09-17 09:17:19
- Modify Date: 2024-01-09 19:30:40
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AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively.
| Name | Benzeneacetamide, 4-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[1-(1-methylethyl)-1H-pyrazol-4-yl] |
|---|---|
| Synonyms |
2-{4-[(6,7-Dimethoxy-4-quinazolinyl)oxy]phenyl}-N-(1-isopropyl-1H-pyrazol-4-yl)acetamide
Benzeneacetamide, 4-[(6,7-dimethoxy-4-quinazolinyl)oxy]-N-[1-(1-methylethyl)-1H-pyrazol-4-yl]- AZD2932 |
| Description | AZD2932 is a potent and multi-targeted kinase inhibitor VEGFR2, PDGFβ, Flt-3 and c-Kit with IC50s of 8, 4, 7 and 9 nM in cell assay, respectively. |
|---|---|
| Related Catalog | |
| Target |
VEGFR2:8 nM (IC50) PDGFRβ:4 nM (IC50) FLT3:7 nM (IC50) c-Kit:9 nM (IC50) |
| In Vitro | AZD2932 has a potent and balanced profile against PDGFβ, VEGFR-2, Flt-3 and c-Kit. It 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)[1]. |
| In Vivo | Twice daily oral dosing (b.i.d.) of AZD2932 10 h apart results in significant tumor growth inhibition of 64% for both 50 and 12.5 mg/kg doses on the day the control animals are terminated. Xenografts bearing non PDGFβ expressing tumor cells are also sensitive to AZD2932 treatment: growth of Calu-6 tumor is inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and and LoVo tumors by 67% at 50 mg/kg b.i.d. This is due AZD2932 potent activity against VEGFR2 as well as a potential effect on pericytes and tumor-associated fibroblasts due to PDGFR a and b inhibition. AZD2932 at 3–50 mg/kg b.i.d. 10 h apart gives 60–80% inhibition of both p-VEGFR2 and p-PDGFβ in a 1:1 ratio[1]. |
| Animal Admin | Mice: To confirm that AZD2932 has similar potency against both PDGFβ and VEGFR-2 phosphorylation, the female nude mice bearing C6 tumors are dosed iv with VEGF-A and PDGFBB 5 min prior to cull and 6 h post last dose of AZD2932 and the lungs excised immediately after. Lung lysates are analyzed by western blot for total and phosphorylated VEGFR-2 and PDGFβ[1]. |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 676.9±55.0 °C at 760 mmHg |
| Molecular Formula | C24H25N5O4 |
| Molecular Weight | 447.486 |
| Flash Point | 363.2±31.5 °C |
| Exact Mass | 447.190643 |
| PSA | 100.39000 |
| LogP | 3.18 |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.629 |
| Storage condition | -20℃ |