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| 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 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) |
| 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. |
| KPT-185 Preparation Products And Raw materials |
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