Molecular Formula | C23H16F3N3O3 |
Molar Mass | 439.39 |
Density | 1.432±0.06 g/cm3(Predicted) |
Boling Point | 541.2±50.0 °C(Predicted) |
Solubility | DMSO: 7.75 mg/mL |
pKa | 12.65±0.70(Predicted) |
Storage Condition | -20℃ |
In vitro study | BFH772 effectively targets VEGFR2 with an IC50 of 3 nM. The effectiveness of FLK-1, FLT-1 and FLT-4 was 500 times lower than that of VEGFR2. In addition to VEGFR2, it can target B- RAF, RET and TIE-2, although they are more than 40-fold less effective than VEGFR2. BFH772 inhibits ligand-induced autophosphorylation of RET, PDGFR, and KIT kinases with an IC50 of 30-160 nM. |
In vivo study | Daily oral administration of 3 mg/kg of BFH772 was effective in inhibiting melanoma growth (54-90% reduction for primary tumors; 71-96% reduction for metastases). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.276 ml | 11.379 ml | 22.759 ml |
5 mM | 0.455 ml | 2.276 ml | 4.552 ml |
10 mM | 0.228 ml | 1.138 ml | 2.276 ml |
5 mM | 0.046 ml | 0.228 ml | 0.455 ml |
biological activity | BFH772 is a new, effective and orally available VEGFR2 inhibitor with IC50 of 3 nM. |
target | TargetValue VEGFR2 (Cell-free say) 3 nM |
Target | Value |
VEGFR2 (Cell-free assay) | 3 nM |
in vitro study | BFH772 effectively targets VEGFR2 with IC50 of 3 nM. However, the effectiveness of FLK-1, FLT-1 and FLT-4 is 500 times lower than that of VEGFR2. In addition to VEGFR2, it can also target B- RAF, RET and TIE-2, although its effectiveness is more than 40 times lower than VEGFR2. BFH772 inhibits ligand-induced autophosphorylation of RET, PDGFR, and KIT kinase with an IC50 of 30-160 nM. |
in vivo study | oral administration of 3 mg/kg BFH772 per day can effectively inhibit the growth of melanoma (for primary tumors, reduce 54-90%; For metastatic tumors, reduce 71-96%). |