化合物NVP-ACC789

Name	ACC-789
Synonyms	ACC789 ACC-789 Acc-789 ACC 789 ZK 202650 ZK-202650 NVP-ACC-789 NVP-ACC-789 ACC-789 (NVP-ACC789) N-(3-Bromo-4-methylphenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine N-(3-Bromo-4-methylphenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine
CAS	300842-64-2

Molecular Formula	C21H17BrN4
Molar Mass	405.29
Density	1.441
Storage Condition	Room Temprature
In vitro study	The enzymatic kinase assays demonstrate that NVP-ACC789 is an inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC 50 s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively. In VEGF-treated cultures, addition of the VEGFR-2 inhibitor NVP-ACC789 reduces BME cell number to baseline levels from 1 μM. Likewise, bFGF-induced BME cell proliferation is reduced markedly by NVP-ACC789 from 1 to 10 μM, without however reaching basal levels. NVP-ACC789 is found to be a potent inhibitor of VEGF-induced HUVE cell proliferation with an IC 50 of 1.6 nM. NVP-ACC789 also completely inhibits VEGF-induced BME and BAE cell invasion and VEGF-C-induced BAE cell invasion. The inhibition is dose-dependent in both cell types with a maximal effect from 1 μM.
In vivo study	NVP-ACC789 which is given in daily oral doses for 6 days blocks VEGF-induced angiogenesis in a dose-dependent manner. NVP-ACC789 also inhibits the response to bFGF to some extent, but the dose-response curve is not linear for NVP-ACC789.