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  • DC Chemicals Limited
  • China
  • Product Name: AZD2932
  • Price: $700.0/100mg $1300.0/250mg $2500.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

883986-34-3

883986-34-3 structure
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
  • 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

[1]. Plé PA, et al. Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases. Bioorg Med Chem Lett. 2012 Jan 1;22(1):262-6.

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℃