1421919-75-6

Basic information

• Product Name: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-
• Synonyms: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-;KPT-276;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
• CAS NO: 1421919-75-6
• Molecular Formula: C₁₆H₁₀F₈N₄O
• Molecular Weight: 426.2640256
• EINECS: -0
• Product Categories: API;Inhibitors
• Mol File: 1421919-75-6.mol
• Article Data: 2

Chemical Properties

• Boiling Point: 477.2±55.0 °C(Predicted)
• Appearance: /
• Density: 1.56±0.1 g/cm3(Predicted)
• Solubility: insoluble in EtOH; insoluble in H2O; ≥19.85 mg/mL in DMSO
• PKA: 0.59±0.50(Predicted)
• CAS DataBase Reference: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-(CAS DataBase Reference)
• NIST Chemistry Reference: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-(1421919-75-6)
• EPA Substance Registry System: (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-(1421919-75-6)

Safety Data

• Hazardous Substances Data: 1421919-75-6(Hazardous Substances Data)

Usage

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.

Upstream product

• 288315-03-7 3,3-difluoroazetidine hydrochloride 
• 1388842-44-1 (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid 
• 317319-15-6 3,5-bis(trifluoromethyl)benzothioamide 
• 27126-93-8 3,5-bis(trifluoromethyl)benzonitrile 
• 1333152-22-9 (Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate 
• 1333154-10-1 3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazole 
• 1421920-40-2 (Z)-1-(3,3-difluoroazetidin-1-yl)-3-iodoprop-2-en-1-one 

Relevant articles and documents

NUCLEAR TRANSPORT MODULATORS AND USES THEREOF

The present invention relates to compounds of Structural Formulas (I), (II) and (III): or their pharmaceutically acceptable salts; pharmaceutical compositions comprising the compounds of Structural Formulas (I), (II) and (III); and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRMl activity. The values for the variables in Structural Formulas (I), (II) and (III) are as described and defined herein.