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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 47 mg/mL (Need ultrasonic and warming)|
|Related VEGFR/PDGFR Products|
Pamufetinib (TAS-115) is a highly potent inhibitor of both C-MET and VEGFR, with IC50 of 30 nM and 32 nM against recombinant VEGFR2 and VEGFR, respectively.
Chiauranib (CS2164) is a multi-target inhibitor with oral activity against tumor angiogenesis. Chiauranib effectively inhibits angiogenesis-associated kinases (VEGFR1, VEGFR2, VEGFR3, PDGFRα and c-Kit), mitosis-associated kinase Aurora B, and chronic inflammation-associated kinase CSF-1R,IC50 The value is 1-9 nM. Chiauranib has a strong anti-cancer effect.
TAS-115 (Pamufetinib) mesylate inhibited the kinase activity of both VEGFR2 and MET and their signal-dependent cell growth as strongly as other known VEGFR or MET inhibitors.
Ningetinib is a potent, orally bioavailable tyrosine kinase inhibitor for Axl, VEGFR2 and c-Met with IC50 values of <1.0, 1.9 and 6.7 nM, respectively.
Tanshinone IIA suppresses angiogenesis by targeting the protein kinase domains of VEGF/VEGFR2. *The compound is unstable in solutions, freshly prepared is recommended.
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