KPT-185CRM1 inhibitor,selective and irrversible CAS# 1333151-73-7 |
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Quality Control & MSDS
3D structure
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| Cas No. | 1333151-73-7 | SDF | Download SDF |
| PubChem ID | 53495165 | Appearance | Powder |
| Formula | C16H16F3N3O3 | M.Wt | 355.31 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble in DMSO > 10 mM | ||
| Chemical Name | propan-2-yl (Z)-3-[3-[3-methoxy-5-(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]prop-2-enoate | ||
| SMILES | CC(C)OC(=O)C=CN1C=NC(=N1)C2=CC(=CC(=C2)OC)C(F)(F)F | ||
| Standard InChIKey | NLNGWFLRRRYNIL-PLNGDYQASA-N | ||
| Standard InChI | InChI=1S/C16H16F3N3O3/c1-10(2)25-14(23)4-5-22-9-20-15(21-22)11-6-12(16(17,18)19)8-13(7-11)24-3/h4-10H,1-3H3/b5-4- | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | KPT-185 is a selective inhibitor of CRM1. | |||||
| Targets | CRM1 | |||||
KPT-185 Dilution Calculator
KPT-185 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.8144 mL | 14.0722 mL | 28.1444 mL | 56.2889 mL | 70.3611 mL |
| 5 mM | 0.5629 mL | 2.8144 mL | 5.6289 mL | 11.2578 mL | 14.0722 mL |
| 10 mM | 0.2814 mL | 1.4072 mL | 2.8144 mL | 5.6289 mL | 7.0361 mL |
| 50 mM | 0.0563 mL | 0.2814 mL | 0.5629 mL | 1.1258 mL | 1.4072 mL |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2814 mL | 0.5629 mL | 0.7036 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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].
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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Ribosomal Biogenesis and Translational Flux Inhibition by the Selective Inhibitor of Nuclear Export (SINE) XPO1 Antagonist KPT-185.[Pubmed:26340096]
PLoS One. 2015 Sep 4;10(9):e0137210.
Mantle cell lymphoma (MCL) is an aggressive B-cell lymphoma characterized by the aberrant expression of several growth-regulating, oncogenic effectors. Exportin 1 (XPO1) mediates the nucleocytoplasmic transport of numerous molecules including oncogenic growth-regulating factors, RNAs, and ribosomal subunits. In MCL cells, the small molecule KPT-185 blocks XPO1 function and exerts anti-proliferative effects. In this study, we investigated the molecular mechanisms of this putative anti-tumor effect on MCL cells using cell growth/viability assays, immunoblotting, gene expression analysis, and absolute quantification proteomics. KPT-185 exhibited a p53-independent anti-lymphoma effect on MCL cells, by suppression of oncogenic mediators (e.g., XPO1, cyclin D1, c-Myc, PIM1, and Bcl-2 family members), repression of ribosomal biogenesis, and downregulation of translation/chaperone proteins (e.g., PIM2, EEF1A1, EEF2, and HSP70) that are part of the translational/transcriptional network regulated by heat shock factor 1. These results elucidate a novel mechanism in which ribosomal biogenesis appears to be a key component through which XPO1 contributes to tumor cell survival. Thus, we propose that the blockade of XPO1 could be a promising, novel strategy for the treatment of MCL and other malignancies overexpressing XPO1.
