Molecular Formula | C25H17F2N5O3S |
Molar Mass | 505.5 |
Density | 1.45 |
Melting Point | 187-189℃ |
Boling Point | 715.6±70.0 °C(Predicted) |
Solubility | Soluble in DMSO, not in water |
Appearance | Solid |
Color | White to Pale Yellow |
pKa | 6.23±0.40(Predicted) |
Storage Condition | Refrigerator |
Use | Omipalisib (GSK2126458) is an orally effective, highly selective PI3K inhibitor that inhibits the activity of p110α/β/δ/γ,mTORC1/2 with Ki values of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM, respectively. |
In vitro study | GSK2126458 potently inhibits the common activating mutant of p110α(E542K, e5445k, and H1047R) found in human cancer cells with Ki of 8 pM, 8 pM, and 9 pM, respectively. GSK2126458 significantly reduced the level of T47D and BT474 cells by pAKT-S473, with IC50 of 0.41 nM and 0.18 nM, respectively. Furthermore, GSK2126458 acts on a variety of cell lines, including the T47D and BT474 breast cancer cell lines, causing the cell cycle to stop at G1 phase and inhibiting cell proliferation with IC50 of 3 nM and 2.4 nM, respectively. |
In vivo study | The effect of GSK2126458 on BT474 human xenograft tumor model was reduced by pAKT-S473, which was dose-dependent, and the effect was inhibited by 300 μg /kg low dose. In addition, GSK2126458 acts on four preclinical species (mouse, rat, dog, and monkey) with low blood clearance and good oral bioavailability. |
HS Code | 29350090 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.978 ml | 9.891 ml | 19.782 ml |
5 mM | 0.396 ml | 1.978 ml | 3.956 ml |
10 mM | 0.198 ml | 0.989 ml | 1.978 ml |
5 mM | 0.04 ml | 0.198 ml | 0.396 ml |