Molecular Formula | C17H14ClF2N3O3S |
Molar Mass | 413.83 |
Density | 1.55 |
Melting Point | 230-233oC |
Solubility | DMSO (Slightly), Methanol (Slightly, Heated) |
Appearance | Orange-yellow solid |
Color | White to Off-White |
pKa | 6.20±0.10(Predicted) |
Storage Condition | +2C to +8C |
Refractive Index | 1.645 |
In vitro study | PLX-4720 high affinity and activity B- Raf10 μm PLX-4720 treatment of PTEN |
In vivo study | PLX-4720 8505c tumors treated with 20 mg/kg daily oral administration of dependent B- Raf PLX-4720 at 30 mg/kg daily significantly inhibited tumor growth by more than 90%, distant lung metastases were also significantly reduced. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.416 ml | 12.082 ml | 24.165 ml |
5 mM | 0.483 ml | 2.416 ml | 4.833 ml |
10 mM | 0.242 ml | 1.208 ml | 2.416 ml |
5 mM | 0.048 ml | 0.242 ml | 0.483 ml |
biological activity | PLX-4720 is a potent, selective B- RafV600E inhibitor with an IC50 of 13 nM, acting on c-Raf-1(Y340D and Y341D mutants) was moderately effective, acting on B- RafV600E being 10-fold more selective than acting on wild-type B- Raf. PLX-4720 is a potent, selective B- RafV600E inhibitor with an IC50 of 13 nM in a cell-free assay, equally effective at c-Raf-1(Y340D and Y341D mutants), the selectivity was 10-fold higher for B- RafV600E than for wild-type B- Raf. |
Target | Value |
C-Raf-1 (Y340D/Y341D) (Cell-free assay) | 6.7 nM |
B-Raf (V600E) (Cell-free assay) | 13 nM |
BRK (Cell-free assay) | 130 nM |
B-Raf (Cell-free assay) | 160 nM |