Molecular Formula | C25H20N4O3 |
Molar Mass | 424.45 |
Density | 1.40±0.1 g/cm3(Predicted) |
Boling Point | 701.9±60.0 °C(Predicted) |
Solubility | DMSO: ≥ 40 mg/mL |
pKa | 10.51±0.70(Predicted) |
Storage Condition | -20℃ |
In vitro study | In living cells, RBC8 reduces RalA activation by inducing chemical shift changes in RalB-GDP. In Ral-dependent H2122 and H358, RBC8 caused anchorage-independent growth inhibition with IC50 of 3.5 µm and 3.4 µm, respectively. |
In vivo study | In mice bearing H358 xenografts, RBC8 (50 mg/kg I. p.) inhibited tumor growth through specific inhibition of RalA and RalB. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.356 ml | 11.78 ml | 23.56 ml |
5 mM | 0.471 ml | 2.356 ml | 4.712 ml |
10 mM | 0.236 ml | 1.178 ml | 2.356 ml |
5 mM | 0.047 ml | 0.236 ml | 0.471 ml |
biological activity | RBC8 is a selective GTPases RalA and RalB inhibitor, there was no inhibition of GTPases Ras and RhoA by inhibiting the binding of Ral to its effector RALBP1. |