883986-34-3

Usage

Uses

Used in Pharmaceutical Industry:
AZD 2932 is used as a therapeutic agent for inhibiting the activity of VEGFR-2 and PDGFR, which play crucial roles in angiogenesis and cell proliferation. This makes it a potential candidate for the treatment of various diseases, including cancer, where these pathways are often dysregulated.
Used in Cancer Treatment:
AZD 2932 is used as an anti-cancer agent for targeting the VEGFR-2 and PDGFR pathways, which are involved in tumor angiogenesis and growth. By inhibiting these pathways, AZD 2932 can help limit the supply of nutrients and oxygen to the tumor, thereby slowing down or stopping its growth and progression.
Used in Angiogenesis Inhibition:
AZD 2932 is used as an angiogenesis inhibitor, as it targets the VEGFR-2 pathway, which is essential for the formation of new blood vessels. Inhibiting this pathway can prevent the growth of new blood vessels that supply tumors with nutrients and oxygen, thus limiting their growth and spread.
Used in Cell Proliferation Regulation:
AZD 2932 is used as a regulator of cell proliferation, as it targets the PDGFR pathway, which is involved in cell growth and division. By inhibiting this pathway, AZD 2932 can help control the uncontrolled cell growth that is characteristic of many diseases, including cancer.

Biological Activity

azd2932 is a potent inhibitor for multiple protein tyrosine kinases (ic50 = 8 nm, 4 nm, 7 nm, and 9 nm for vegfr-2, pdgfrβ, flt-3, and c-kit, respectively.) [1]vegfr are receptors for vascular endothelial growth factor and belong to receptor tyrosine kinases. it mediates in various cellular functions, including endothelial proliferation, migration, survival, tubular morphogenesis and sprouting. pdgfr are platelet-derived growth factor receptors that exhibit intracellular tyrosine kinase activity. it involves in embryonic development, angiogenesis, proliferation and differentiation etc.azd2932 has a potent and balanced profile against pdgfr, vegfr-2, flt-3 and c-kit (ic50: 0.009). it also has a good fraction unbound between 3.3% free in human and 7.0% in dog sera and has no activity against herg. [1]in female nude mice bearing c6 tumors, azd2932 treatment at 3–50 mg/kg b.i.d. 10 h apart give 60–80% inhibition of both p-vegfr-2 and p-pdgfrb in a 1:1 ratio. [1]

references

1. plé pa, jung f, ashton s, hennequin l 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.