343787-29-1

CP 673451 is a potent PDGFR-β inhibitor with an IC50 of 1 nM.

ChEBI: 1-[2-[5-(2-methoxyethoxy)-1-benzimidazolyl]-8-quinolinyl]-4-piperidinamine is an aminoquinoline.

cp-673451 is a potent inhibitor of pdgfr with ic50 value of 10nm and 1nm for pdgfr-α and pdgfr-β, respectively [1].cp-673451 is an atp-competitive inhibitor and is investigated to treat for cancer. it is highly selective against pdgfr-α and pdgfr-β over a variety of other kinases such as vegfr-1, vegfr-2, lck, tie-2 and egfr. in pae-β cells, cp-673451 inhibits pdgfr-β with ic50 value of 6.4nm. cp-673451 also inhibits c-kit with ic50 value of 1.1μm in h526 cells. in rat c6 glioblastoma xenograft models, a single oral dose of 50mg/kg cp-673451 reduces > 50% phosphorylation of pdgfr-β for 4 hours. in addition, cp-673451 is found to inhibit pdgf-bb-induced angiogenesis in a sponge angiogenesis model. furthermore, cp-673451 inhibits the tumor growth in colo205, ls174t, h460, and u87mg xenograft models. it also reduces the microvessel density of colo205 xenografts [1].

PDGFRβ

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[1] roberts w g, whalen p m, soderstrom e, et al. antiangiogenic and antitumor activity of a selective pdgfr tyrosine kinase inhibitor, cp-673,451. cancer research, 2005, 65(3): 957-966.