KPT-185

Alias: KPT-185;KPT185;KPT 185
Cat No.:V1682 Purity: ≥98%
This product has been discontinued.
KPT-185 Chemical Structure CAS No.: 1333151-73-7
Product category: Potassium Channel
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
ln Vivo

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.
Animal Protocol


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.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H16F3N3O3
Molecular Weight
355.31
CAS #
1333151-73-7
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
Synonyms
KPT-185;KPT185;KPT 185
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 71 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol: 71 mg/mL (199.8 mM)
Solubility (In Vivo)
N/A
 (Please use freshly prepared in vivo formulations for optimal results.)
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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Biological Data
  • KPT-185

    KPT SINEs induce cancer cell selective growth inhibition and apoptosis. Gastroenterology. 2013 Feb;144(2):447-56.
  • KPT-185

    KPT-185 induces nuclear localization of different TSPs including PAR-4 in cancer selective manner. Gastroenterology. 2013 Feb;144(2):447-56.
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