KPT-185

KPT-185 Basic information
Product Name:KPT-185
Synonyms:2-Propenoic acid, 3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-, 1-methylethyl ester, (2Z)-;(2Z)-3-[3-[3-Methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 1-methylethyl ester KPT185;KPT-185;(2Z)-3-[3-[3-Methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 1-methylethyl ester;KPT-185, >=98%;KPT-185;KPT185;(Z)-Isopropyl 3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate;CS-844
CAS:1333151-73-7
MF:C16H16F3N3O3
MW:355.31
EINECS:
Product Categories:Inhibitors
Mol File:1333151-73-7.mol
KPT-185 Structure
KPT-185 Chemical Properties
Boiling point 458.8±55.0 °C(Predicted)
density 1.29±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility insoluble in H2O; ≥17.77 mg/mL in DMSO; ≥25.2 mg/mL in EtOH
form solid
pka0.47±0.50(Predicted)
Safety Information
MSDS Information
KPT-185 Usage And Synthesis
UsesKPT185 acts as a novel CRM1 inhibitor used in the treatment of acute myeloid leukemia.
Biological Activitykpt-185 is a selective and irreversible inhibitor of chromosome maintenance protein 1 (crm1) with ic50 values of 100-500nm [1].crm1 is an important nuclear protein export receptor. blocking crm1-mediated nuclear export can result in the suppression of tumors. as an inhibitor of crm1, kpt-185 binds crm1within the cys528 site and prevents crm1from interacting with tumor-suppressor proteins. in the in vitro studies on aml cell lines, kpt-185 inhibits proliferation of a variety of leukemia cells with ic50 values ranging from 100nm to 500nm. it induces cell-cycle arrest at g1 and induces apoptosis. kpt-185 also strongly affects cell colony formation. in addition, the inhibition of crm1 caused by kpt-185 induces differentiation of aml blast. besides that, kpt-185 is also found to inhibit proliferation and induce apoptosis of pancreatic cancer cells including colo-357, hpac and bxpc-3 [1, 2].
targetCRM1
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] azmi a s, aboukameel a, bao b, et al. selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice. gastroenterology, 2013, 144(2): 447-456.
KPT-185 Preparation Products And Raw materials
KPT-330 Nutlin-3 Trametinib Dabrafenib PD 0325901 (Z)-3-(3-(3,5-bis(trifluoroMethyl)phenyl)-1H-1,2,4-triazol-1-yl)-1-(3,3-

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