Name | Selinexor (KPT-330) |
Synonyms | KPT-330 Aloradine Selinexor KPT330,Selinexor KPT-330,Selinexor Selinexor (KPT-330) (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide (2Z)-3-[3-[3,5-Bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 2-(2-pyrazinyl)hydrazide 2-Propenoic acid, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 2-(2-pyrazinyl)hydrazide, (2Z)- |
CAS | 1393477-72-9 |
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 |