Size | Price | Stock | Qty |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
This product has been discontinued. KPT-185 (KPT185; KPT 185) is an irreversible and selective CRM1 (Chromosomal Maintenance 1, also known as Exportin 1 or XPO1) inhibitor with potential antitumor activity. In 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.
ln Vitro |
KPT-185 produces a considerable drop in CRM1 protein levels and a significant increase of p53 in the nucleus of MV4-11 and OCI-AML3 cells [1]. KPT-185 (1-1000 nM; 72 h) strongly decreases the proliferation of HPB-ALL, Jurkat, CCRF-CEM, MOLT-4, KOPTK1, and LOUCY cells, with an IC50 of 16-395 nM [4]. KPT-185 causes cell cycle arrest in the G1 phase of MOLT-4 cell lines [4].
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ln Vivo |
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Cell Assay |
Cell Viability Assay[4]
Cell Types: HPB-ALL, Jurkat, CCRF-CEM, MOLT-4, KOPTK1, LOUCY cells Tested Concentrations: 1, 10, 100, 1000 nM Incubation Duration: 72 hrs (hours) Experimental Results: The growth of those lines was dramatically decreased with IC50s of 16–395 nM after 72 h of exposure. |
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Animal Protocol |
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References |
[1]. Ranganathan P, et al. Preclinical activity of a novel CRM1 inhibitor in acute myeloid leukemia. Blood. 2012 Aug 30;120(9):1765-73.
[2]. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activityin preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27. [3]. Zhang K, et al. Novel selective inhibitors of nuclear export CRM1 antagonists for therapy in mantle cell lymphoma. Exp Hematol. 2013 Jan;41(1):67-78.e4. [4]. Salas Fragomeni RA, et al. CRM1 and BRAF inhibition synergize and induce tumor regression in BRAF-mutant melanoma. Mol Cancer Ther. 2013 Jul;12(7):1171-9. |
Molecular Formula |
C16H16F3N3O3
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Molecular Weight |
355.31
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CAS # |
1333151-73-7
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC(C1=C([H])C(=C([H])C(C2N=C([H])N(/C(/[H])=C(\[H])/C(=O)OC([H])(C([H])([H])[H])C([H])([H])[H])N=2)=C1[H])OC([H])([H])[H])(F)F
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (7.04 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.04 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.8144 mL | 14.0722 mL | 28.1444 mL | |
5 mM | 0.5629 mL | 2.8144 mL | 5.6289 mL | |
10 mM | 0.2814 mL | 1.4072 mL | 2.8144 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.