AZD2932

SKU: orb1223750

Description

AZD2932 is a new series of quinazoline ether inhibitor which potently inhibits VEGFR-2 and PDGFR with IC50s of 4 nM/8 nM/ 7 nM for PDGFRβ/VEGFR-2/Flt-3.

Key Properties

• CAS Number: 883986-34-3
• MW: 447.49
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₅N₅O₄
• SMILES: O=C(NC1=CN(C(C)C)N=C1)CC2=CC=C(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)C=C2
• Target: c-Kit
• Solubility: Ethanol: 5 mg/mL warmed (11.17 mM); DMSO: 89 mg/mL warmed (198.88 mM)

Bioactivity

• 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.
• 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).

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AZD2932 | AZD 2932 | AZD-2932

Quick Database Links

Gene Symbol

c-Kit