| Identification | Back Directory | [Name]
KPT-185 | [CAS]
1333151-73-7 | [Synonyms]
CS-844
KPT-185
KPT-185, >=98%
KPT-185;KPT185
KPT-185 USP/EP/BP
(Z)-Isopropyl 3-(3-(3-methoxy-5-(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)acrylate
(2Z)-3-[3-[3-Methoxy-5-(trifluoromethyl)phenyl]-1H-1,2,4-triazol-1-yl]-2-propenoic acid 1-methylethyl ester
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 | [Molecular Formula]
C16H16F3N3O3 | [MDL Number]
MFCD25976761 | [MOL File]
1333151-73-7.mol | [Molecular Weight]
355.312 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [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 | [storage]
Store at -20°C | [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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| Company Name: |
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 +86-13986109188 | +86-15623472865 | +81-08033611988 |
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