| Molecular Formula | C17H11F6N7O |
| Molar Mass | 443.31 |
| Density | 1.55±0.1 g/cm3(Predicted) |
| Solubility | Soluble in DMSO (up to at least 25 mg/ml). or in Ethanol (up to at least 25 mg/ml) |
| Appearance | solid |
| Color | Off-white |
| pKa | 9.74±0.43(Predicted) |
| Storage Condition | -20°C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months. |
| Physical and Chemical Properties | Bioactive Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2. |
| Target | Target Value CRM1 (Cell-free assay) |
| In vitro study | KPT-330, as a clinical candidate for KPT-185, has a similar effect on the survival of T-ALL cells and rapidly triggers an apoptotic response. KPT-330 also reduced MOLT-4,Jurkat,HBP-ALL,KOPTK-1,SKW-3, and DND-41 cell line growth with an IC50 of 34-203 nM. |
| In vivo study | In vivo, KPT-330 significantly inhibited the growth of T-ALL cells (MOLT-4) and AML cells (MV4-11), with little toxicity to normal hematopoietic cells. KPT-330 treatment of SCID mice with diffuse human multiple myeloma (MM) bone lesions inhibits MM-induced osteolysis and prolongs life. In addition, KPT-330 directly impaired osteoclast formation and bone resorption by inhibiting RANKL-induced NF-κB and NFATc1, with minimal effects on osteoblasts and BMSCs. |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.256 ml | 11.279 ml | 22.558 ml |
| 5 mM | 0.451 ml | 2.256 ml | 4.512 ml |
| 10 mM | 0.226 ml | 1.128 ml | 2.256 ml |
| 5 mM | 0.045 ml | 0.226 ml | 0.451 ml |