(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Chemical Properties

Boiling point:

477.2±55.0 °C(Predicted)

Density 

1.56±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

insoluble in EtOH; insoluble in H2O; ≥19.85 mg/mL in DMSO

form 

solid

pka

0.59±0.50(Predicted)

(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Usage And Synthesis

Description

KPT-276 is an orally bioavailable inhibitor of Exportin 1 (XPO1/CRM1) with anticancer activity. In vivo, KPT-276 (150 mg/kg) increases survival and reduces spleen weight and white blood cell count in an MV4-11 acute myeloid leukemia (AML) mouse xenograft model. It also reduces tumor volume and increases survival in a BT 145 glioblastoma mouse xenograft model when administered at a dose of 75 mg/kg.

References

[1]. ranganathan p, yu x, na c, et al. preclinical activity of a novel crm1 inhibitor in acute myeloid leukemia. blood, 2012, 120(9): 1765-1773.
[2]. schmidt j, braggio e, kortuem km, et al. genome-wide studies in multiple myeloma identify xpo1/crm1 as a critical target validated using the selective nuclear export inhibitor kpt-276. leukemia, 2013, 27(12): 2357-2365.

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