Molecular Formula | C17H10F6N6O |
Molar Mass | 428.3 |
Density | 1.57±0.1 g/cm3(Predicted) |
Boling Point | 574.4±60.0 °C(Predicted) |
Solubility | DMSO: 4.72 mg/mL |
pKa | 13.06±0.50(Predicted) |
Storage Condition | -20℃ |
In vitro study | In cell viability assays, KPT-8602 were potent inhibitors of AML cells. It inhibits XPO1/cargo interaction and nuclear export, induces apoptosis in primary CLL cells and significantly inhibits proliferation of diffuse large B- cell lymphoma cell lines. |
In vivo study | KPT-8602 has Oral activity, and selinexor has similar pharmacokinetic activity, but the blood brain barrier penetration is significantly reduced. Toxicity tests in rats and monkeys showed that KPT-8602 was safe and well tolerated, possibly due to its inability to penetrate the blood-brain barrier into the central nervous system, anorexia, restlessness, there was a decrease in the symptoms of weight loss. KPT-8602 had better anti-leukemic activity and better tolerability in the AML PDX model. In the AML-CN model, almost complete elimination was achieved for human AML cells. KPT-8602 has little toxicity to normal hematopoietic stem cells and progenitor cells. After repeated dosing, KPT-8602 did not accumulate in plasma and prolonged the survival of the human leukemia xenograft model. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.335 ml | 11.674 ml | 23.349 ml |
5 mM | 0.467 ml | 2.335 ml | 4.67 ml |
10 mM | 0.233 ml | 1.167 ml | 2.335 ml |
5 mM | 0.047 ml | 0.233 ml | 0.467 ml |