(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- 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;KPT276; KPT 276;(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;CS-1100;(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- USP/EP/BP
CAS:1421919-75-6
MF:C16H10F8N4O
MW:426.26
EINECS:
Product Categories:API;Inhibitors
Mol File:1421919-75-6.mol
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Structure
(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
pka0.59±0.50(Predicted)
Safety Information
MSDS Information
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Usage And Synthesis
DescriptionKPT-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.
(Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3- Preparation Products And Raw materials
Olaparib Verdinexor (KPT-335) KPT-330 (Z)-isopropyl 3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate 2-Propenoic acid, 3-iodo-, 1-methylethyl ester, (2Z)- KPT-185 Ribociclib (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylic acid BIX 02189 Bosutinib 3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazole KPT-330, (E)-RN PD 173074

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