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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.
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| 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.
| Molecular Weight | 405.29 |
| Formula | C21H17BrN4 |
| CAS Number | 300842-64-2 |
| Purity | >98% |
| Solubility | DMSO: ≥ 47 mg/mL (Need ultrasonic and warming) |
| Storage | at -20°C |
| Related VEGFR/PDGFR Products |
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| Pamufetinib
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
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 mesylate
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
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
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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