Name | Verdinexor (KPT-335) |
Synonyms | CS-1798 KPT-335 Verdinexor Verdinexor(KPT-335) Verdinexor (KPT-335) Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin- (KPT335)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyridin-2-yl)acrylohydrazide (2Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]- 2-propenoic acid-2-(2-pyridinyl)hydrazide (2Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N -(pyridin-2-yl)prop-2-enehydrazide Verdinexor(KPT-335) |
CAS | 1392136-43-4 |
Molecular Formula | C18H12F6N6O |
Molar Mass | 442.32 |
Density | 1.49±0.1 g/cm3(Predicted) |
pKa | 10.04±0.43(Predicted) |
Storage Condition | -20℃ |
In vitro study | Verdinexor inhibits the viability of Jurkat, OCI-Ly3, OCI-Ly10, and CLBL1 cells with IC50 of 0.3 nM, 2.1 nM, 41.8 nM, and 8.5 nM respectively. KPT-335 also induces apoptosis in CLBL1 cells and primary canine DLBCL cells that express XPO1 and SINE. Verdinexor potently and selectively inhibits vRNP export and effectively inhibits the replication of various influenza virus A and B strains, including pandemic H1N1 virus, high pathogenic H5N1 avian influenza virus, and the recent emerging H7N9 strain. Verdinexor inhibited the activity of Jurkat,OCI-Ly3,OCI-Ly10, and CLBL1 cells with an IC50 of 0.3 nM,2.1 nM,41.8 nM, and 8.5 nM, respectively. KPT-335 also induced apoptosis in CLBL1 and primary canine DLBCL cells expressing XPO1 and SINE. Verdinexor selectively potently inhibits vRNP export and also potently inhibits various influenza Virus A and B strains, including pandemic H1N1 Virus, highly pathogenic H5N1 avian influenza Virus, and more recently the H7N9 strain. |
In vivo study | Verdinexor (25 mg/kg twice daily, p.o.) reduces proinflammatory cytokine expression in the lung, produces in vivo antiviral activity by reducing lung virus titers, and thus reduces pulmonary disease pathogenesis and death associated with lethal influenza A virus challenge. In autosomal-dominant polycystic kidney disease model, Verdinexor (5 mg/kg, I .p.) attenuates cyst growth via inhibition of XPO1. Verdinexor (25 mg/kg twice daily, p.o.) reduces the expression of pro-inflammatory cytokines in the lungs, produces anti-Virus activity in vivo by reducing lung Virus titers, and thus reduces lung disease associated with lethal influenza A A Virus by Incidence Rate and Mortality Rate. In an autosomal dominant polycystic kidney disease model, Verdinexor (5 mg/kg, I. p.) attenuates cyst growth by inhibiting xpo1. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.261 ml | 11.304 ml | 22.608 ml |
5 mM | 0.452 ml | 2.261 ml | 4.522 ml |
10 mM | 0.226 ml | 1.13 ml | 2.261 ml |
5 mM | 0.045 ml | 0.226 ml | 0.452 ml |