AZD2932 (883986-34-8) Description:
AZD-2932 is a high affinity inhibitor of VEFGR-2 and PDGFR. AZD-2932 has a balanced ~ 1:1 ratio of activity vs both VEGFR-2 and PDGFRβ and shows IC50 values of 8 and 4 nM against the two enzymes, respectively. It is also active on c-Kit and FLT3 with good selectivity on a panel of kinases. The pharmacokinetic behavior and the preclinical antitumor activity in nude mice bearing C6 rat glial tumors indicate that 31 has the potential to become an antiangiogenic agent in the clinic.
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 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.
AZD2932 (883986-34-8) Specifications:
|Synonym||AZD2932; AZD 2932; AZD-2932|
|Molecular Weight||447.495 g/mol|
|Monoisotopic Mass||447.191 g/mol|
|Solubility||DMSO 89 mg/mL (198.89 mM)
Alcohol 5 mg/mL (11.17 mM)
|Shelf life||>2 years if stored properly|
|Handling||Protect from air and moisture|
|Application||affinity inhibitor of VEFGR-2 and PDGFR|