Verdinexor
Based on 3 publication(s) in Google Scholar
Verdinexor (KPT-335) is an orally active inhibitor for selective inhibitor of nuclear export (SINE). Verdinexor inhibits the respiratory syncytial virus A2 (RSV A2) replication with an IC50 of 0.96 µM. Verdinexor inhibits the function of nuclear export protein Exportin 1 (XPO1/CRM1), inhibiting pro-inflammatory responses. Verdinexor exhibits antitumor effciency.
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- Purity : 99.94%
- CAS No.: 1392136-43-4
- 화학식: C18H12F6N6O
- 분자량:442.32
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Verdinexor
More
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Jurkat | EC50 |
27 nM
Compound: 16; KPT-335
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Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
Cytotoxicity against human Jurkat cells incubated for 24 hrs by celltiter glo assay
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[PMID: 39005064] |
| MDCK | CC50 |
31.77 μM
Compound: Verdinexor
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Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay
Cytotoxicity against MDCK cells assessed as cell death after 72 hrs by MTT assay
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[PMID: 30753063] |
| SH-SY5Y | IC50 |
0.3 μM
Compound: 12; KPT-335
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Antiproliferative activity against human SH-SY5Y cells by CCK-8 assay
Antiproliferative activity against human SH-SY5Y cells by CCK-8 assay
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[PMID: 34669417] |
| SK-N-BE(2) | IC50 |
1.4 μM
Compound: 12; KPT-335
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Antiproliferative activity against human SK-N-BE(2) cells by CCK-8 assay
Antiproliferative activity against human SK-N-BE(2) cells by CCK-8 assay
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[PMID: 34669417] |
In Vitro
Verdinexor (0-10 µM, 72 h) inhibits the proliferation of Jurkat cell and diffuse large B cell lymphoma (DLBCL) cells OCI-Ly3, OCI-Ly10 and CLBL1 with IC50s of 0.3 nM, 2.1 nM, 41.8 nM, and 8.5 nM, respectively[1].
Verdinexor (0-10 µM, 24 h) induces apoptosis in CLBL1 cell and primary canine DLBCL cell[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dog non-Hodgkin lymphoma models[1]
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Dosage:1-2 mg/kg
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Administration:po, twice a week for 4 weeks
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Result:Stabilized or inhibited the tumor progression.
Induced anorexia, weight loss, vomiting, and diarrhea.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1392136-43-4
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Appearance Solid
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분자량 442.32
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화학식 C18H12F6N6O
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Color Light yellow to yellow
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SMILES
O=C(NNC1=NC=CC=C1)/C=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2
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Synonyms
KPT-335
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
XPO1/CRM1 is a promising prognostic indicator for neuroblastoma and represented a therapeutic target by selective inhibitor verdinexor. [Abstract]2021 Aug 12;40(1):255. PMID: 34384466 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
용액&용해도
In Vitro:
DMSO : ≥ 100 mg/mL (226.08 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
순도&문서
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. London CA, et al., Preclinical evaluation of the novel, orally bioavailable Selective Inhibitor of Nuclear Export (SINE) KPT-335 in spontaneous canine cancer: results of a phase I study. PLoS One. 2014 Feb 4;9(2):e87585. [Content Brief]
[2]. Jorquera PA, et al., Verdinexor (KPT-335), a Selective Inhibitor of Nuclear Export, Reduces Respiratory Syncytial Virus Replication In Vitro. J Virol. 2019 Feb 5;93(4):e01684-18. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2608 mL | 11.3040 mL | 22.6081 mL | 56.5202 mL |
| 5 mM | 0.4522 mL | 2.2608 mL | 4.5216 mL | 11.3040 mL | |
| 10 mM | 0.2261 mL | 1.1304 mL | 2.2608 mL | 5.6520 mL | |
| 15 mM | 0.1507 mL | 0.7536 mL | 1.5072 mL | 3.7680 mL | |
| 20 mM | 0.1130 mL | 0.5652 mL | 1.1304 mL | 2.8260 mL | |
| 25 mM | 0.0904 mL | 0.4522 mL | 0.9043 mL | 2.2608 mL | |
| 30 mM | 0.0754 mL | 0.3768 mL | 0.7536 mL | 1.8840 mL | |
| 40 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4130 mL | |
| 50 mM | 0.0452 mL | 0.2261 mL | 0.4522 mL | 1.1304 mL | |
| 60 mM | 0.0377 mL | 0.1884 mL | 0.3768 mL | 0.9420 mL | |
| 80 mM | 0.0283 mL | 0.1413 mL | 0.2826 mL | 0.7065 mL | |
| 100 mM | 0.0226 mL | 0.1130 mL | 0.2261 mL | 0.5652 mL |
Verdinexor Related Classifications
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