| Size | Price | Stock | Qty |
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| Targets |
Eltanexor Z-isomer targets the nuclear export pathway via XPO1 (exportin 1, also known as CRM1). XPO1 is responsible for the nuclear export of tumor suppressor proteins and other regulatory molecules. By blocking XPO1, SINE compounds can restore nuclear localization and function of these proteins. The Z-isomer is the less active form of KPT-8602.
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| ln Vitro |
Eltanexor Z-isomer is the less active isomer of KPT-8602. KPT-8602 is a selective inhibitor of nuclear export (SINE) that specifically blocks XPO1/CRM1-mediated nuclear export. The Z-isomer is used as a reference compound in research to study XPO1 inhibition and the structure-activity relationships of SINE compounds.
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| ln Vivo |
In vivo, Eltanexor Z-isomer is used as a research tool to study XPO1-mediated nuclear export and the effects of SINE compounds. As the less active isomer, it serves as a control or reference compound for comparing the activity of the more active E-isomer. It is used in studies of cellular stress responses, protein homeostasis, and age-related decline.
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| Enzyme Assay |
In vitro binding assays for Eltanexor Z-isomer typically employ purified XPO1/CRM1 protein and measure binding affinity using surface plasmon resonance (SPR) or fluorescence-based assays. Inhibition of XPO1-mediated nuclear export is assessed using reporter constructs containing nuclear export signals (NES) and measuring nuclear/cytoplasmic distribution by fluorescence microscopy or cell fractionation.
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| Cell Assay |
In vitro cellular assays for Eltanexor Z-isomer involve treating cancer cell lines with varying concentrations of the compound (typically 0.01-100 microM range) for 24-72 hours. Readouts include assessment of nuclear export inhibition by measuring the localization of XPO1 cargo proteins, cell viability, and evaluation of downstream signaling pathways affected by nuclear export inhibition.
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| Animal Protocol |
In vivo animal studies for Eltanexor Z-isomer would typically employ xenograft mouse models to compare the activity of the Z-isomer with the more active E-isomer. Animals would be administered the compound via appropriate routes at various doses. Endpoints would include tumor growth inhibition, body weight, survival, and pharmacodynamic biomarkers of XPO1 inhibition.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Eltanexor Z-isomer are characteristic of small molecule SINE compounds. With a molecular weight of 428.29, the compound is a small molecule. PK parameters including half-life, Cmax, Tmax, and AUC would be determined via LC-MS/MS analysis following administration in appropriate animal models.
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| Toxicity/Toxicokinetics |
Eltanexor Z-isomer is a research-grade compound for laboratory use only. As with all research chemicals, standard safety precautions should be observed during handling including appropriate PPE and work in a fume hood. The compound is not intended for human therapeutic use.
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| References |
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| Additional Infomation |
Eltanexor Z-isomer (CAS# 1642300-78-4) is the less active isomer of KPT-8602, a selective inhibitor of nuclear export (SINE) targeting XPO1/CRM1. It is used as a research tool and reference compound for studying XPO1 inhibition. Not for clinical use.
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| Molecular Formula |
C17H10F6N6O
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|---|---|
| Molecular Weight |
428.291323184967
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| Exact Mass |
428.082
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| CAS # |
1642300-78-4
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| Related CAS # |
Eltanexor;1642300-52-4
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| PubChem CID |
117763569
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
2.5
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
30
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N)/C(C1=CN=CN=C1)=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2
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| InChi Key |
JFBAVWVBLRIWHM-MLPAPPSSSA-N
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| InChi Code |
InChI=1S/C17H10F6N6O/c18-16(19,20)11-1-9(2-12(3-11)17(21,22)23)15-27-8-29(28-15)6-13(14(24)30)10-4-25-7-26-5-10/h1-8H,(H2,24,30)/b13-6-
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| Chemical Name |
(Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-2-pyrimidin-5-ylprop-2-enamide
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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 |
| 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) |
DMSO : ~50 mg/mL (~116.74 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (6.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (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 27.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3349 mL | 11.6743 mL | 23.3487 mL | |
| 5 mM | 0.4670 mL | 2.3349 mL | 4.6697 mL | |
| 10 mM | 0.2335 mL | 1.1674 mL | 2.3349 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.
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