| Identification | Back Directory | [Name]
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- | [CAS]
1421919-75-6 | [Synonyms]
KPT-276
CS-1100
KPT276; KPT 276
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- USP/EP/BP
(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
(Z)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one
2-Propen-1-one, 3-[3-[3,5-bis(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-1-(3,3-difluoro-1-azetidinyl)-, (2Z)-
(KPT276)(Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-difluoroazetidin-1-yl)prop-2-en-1-one | [Molecular Formula]
C16H10F8N4O | [MDL Number]
MFCD27937049 | [MOL File]
1421919-75-6.mol | [Molecular Weight]
426.26 |
| Chemical Properties | Back Directory | [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) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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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