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
- Product Categories:
-
- Inhibitors
- Mol File:
- 1333151-73-7.mol
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
- pka
- 0.47±0.50(Predicted)
- color
- White to off-white
KPT-185 Usage And Synthesis
Uses
KPT185 acts as a novel CRM1 inhibitor used in the treatment of acute myeloid leukemia.
Biological Activity
kpt-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].
target
CRM1
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.
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