Molecular Formula | C25H25BrN6O2 |
Molar Mass | 521.41 |
Density | 1.487±0.06 g/cm3(Predicted) |
Solubility | DMSO: 25 mg/mL |
pKa | 8.32±0.40(Predicted) |
Storage Condition | -20℃ |
In vitro study | RS4-11 potently inhibited FLT3 autophosphorylation with an IC50 of <8 nM in FLT3-WT of the MV4-11 cell load and Molm-14 of the FLT3-ITD containing G-749 and cells. In leukemic cells, G-749 showed antiproliferative activity by inducing apoptosis. In BaF3 cell lines stably expressing FLT3-ITD/N676D,FLT3-ITD/F691L,FLT3-D835Y, or FLT3-D835Y/N676D, G-749 showed strong inhibitory activity with IC50 <10 nM, thereby overcoming drug resistance. Of the blast cells in AML patients, G-749 also showed potent anti-leukemic effects. |
In vivo study | G-749 (30 mg/kg p.o.) potently inhibited the FLT3 pathway and significantly inhibited tumor growth in MV4-11 xenografted mice. In an orthogonal model using Molm-14 cell bone marrow transplantation, G-749 (20 mg/kg p.o.) also inhibited tumor growth and improved survival. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.918 ml | 9.589 ml | 19.179 ml |
5 mM | 0.384 ml | 1.918 ml | 3.836 ml |
10 mM | 0.192 ml | 0.959 ml | 1.918 ml |
5 mM | 0.038 ml | 0.192 ml | 0.384 ml |