Molecular Formula | C35H29F3N4O3 |
Molar Mass | 610.62 |
Density | 1.39±0.1 g/cm3(Predicted) |
Boling Point | 857.5±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 32 mg/mL |
pKa | 12.96±0.46(Predicted) |
Storage Condition | -20℃ |
In vitro study | In several human gastric cancer cell lines, KPT-9274 interferes with the PAK4 and NAD biosynthetic pathways, resulting in reduced G2/M transition, induction of apoptosis, and reduced cell invasion and migration. KPT-9274 inhibition of the PAK4 pathway reduces the nuclear localization of β-catenin and the Wnt/β-catenin signaling targets cyclin D1 and c-Myc. |
In vivo study | KPT-9274 administration to an animal model of transplanted tumor with 786-O (VHL-mut) human gastric cancer cells caused a concentration-dependent inhibition of tumor growth without significant toxicity. KPT-9274 also has significant anti-tumor activity in xenograft models transplanted with pancreatic ductal adenocarcinoma and cancer stem cells by subcutaneous injection. KPT-9274 has a favorable pharmacokinetic profile in vivo and is well tolerated in mice, with no toxic effects observed at doses of 200 mg/kg of the drug intravenously or orally. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.638 ml | 8.188 ml | 16.377 ml |
5 mM | 0.328 ml | 1.638 ml | 3.275 ml |
10 mM | 0.164 ml | 0.819 ml | 1.638 ml |
5 mM | 0.033 ml | 0.164 ml | 0.328 ml |