NVP-ACC789, also known as ACC-789 and ZK-202650, is a potent, selective and orally active inhibitor of the VEGF receptor tyrosine kinases with potential anticancer activity. NVP-ACC789 reduces BME cell number to baseline levels from 1 μM. 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, NVP-ACC789 oral doses for 6 days blocks VEGF-induced angiogenesis in a dose-dependent manner.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 47 mg/mL (Need ultrasonic and warming)|
Vascular endothelial growth factor (VEGF) receptor-2 antagonists inhibit VEGF- and basic fibroblast growth factor-induced angiogenesis in vivo and in vitro.
Tille JC, et al. J Pharmacol Exp Ther. 2001 Dec;299(3):1073-85. PMID: 11714897.
|Related VEGFR/PDGFR Products|
Tanshinone IIA suppresses angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. *The compound is unstable in solutions, freshly prepared is recommended.
AC710 is a potent, selective and orally active platelet-derived growth factor receptor-family (PDGFR) kinase inhibitor with potential anticancer activity.
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor.
ODM-203 is an orally available inhibitor of VEGFR and FGFR, with IC50s of 26, 9, 5 nM for VEGFR1, VEGFR2 and VEGFR3, and 11, 16, 6, 35 nM for recombinant FGFR1, FGFR2, FGFR3 and FGFR4, respectively.
MAZ51 is originally synthesized inhibitor of VEGFR-3 (Flt-4) tyrosine kinase, inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2.
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