SP-alkyne
Based on 1 Customer Validation
SP-alkyne is a T cell activation inhibitor probe that covalently binds to and labels Exportin-1 (XPO1) protein in cells. SP-alkyne is an alkyne derivative of SP-100030 (HY-110177). SP-alkyne potently inhibits T cell activation by covalently labeling cysteine residues of XPO1. SP-alkyne inhibits IL-2 production as well as AP-1 and NFAT reporter gene activity. SP-alkyne can be used for research on idiopathic pulmonary fibrosis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.04%
- Fòrmula: C15H6ClF6N3O
- Peso molecular:393.67
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
IL-2 |
In Vitro
SP-alkyne (1 μM; 1 h) covalently labels recombinant human XPO1 protein, and this labeling is blocked by pretreatment with Selinexor (HY-17536)[1].
SP-alkyne (1 μM; 1 h) specifically labels wild-type XPO1 in Jurkat cells expressing wild-type or mutant (C528S) XPO1, but fails to label the C528S mutant protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (female, 8 weeks old)[1]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:i.p.; once daily; 5 days
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Result:In spleen lysates, XPO1 was labeled at 10 mg/kg and 30 mg/kg, with stronger labeling at 30 mg/kg.
In lung lysates, XPO1 was also labeled at 10 mg/kg and 30 mg/kg.
Target engagement with XPO1 in the lung and spleen was dose-dependent.
Chemical Information
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Appearance Solid
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Peso molecular 393.67
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Fòrmula C15H6ClF6N3O
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Color White to off-white
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SMILES
C#CC1=CC(NC(C2=C(C(F)(F)F)N=C(Cl)N=C2)=O)=CC(C(F)(F)F)=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : ≥ 100 mg/mL (254.02 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 (6.35 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.35 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
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| DMSO | 1 mM | 2.5402 mL | 12.7010 mL | 25.4020 mL | 63.5050 mL |
| 5 mM | 0.5080 mL | 2.5402 mL | 5.0804 mL | 12.7010 mL | |
| 10 mM | 0.2540 mL | 1.2701 mL | 2.5402 mL | 6.3505 mL | |
| 15 mM | 0.1693 mL | 0.8467 mL | 1.6935 mL | 4.2337 mL | |
| 20 mM | 0.1270 mL | 0.6350 mL | 1.2701 mL | 3.1752 mL | |
| 25 mM | 0.1016 mL | 0.5080 mL | 1.0161 mL | 2.5402 mL | |
| 30 mM | 0.0847 mL | 0.4234 mL | 0.8467 mL | 2.1168 mL | |
| 40 mM | 0.0635 mL | 0.3175 mL | 0.6350 mL | 1.5876 mL | |
| 50 mM | 0.0508 mL | 0.2540 mL | 0.5080 mL | 1.2701 mL | |
| 60 mM | 0.0423 mL | 0.2117 mL | 0.4234 mL | 1.0584 mL | |
| 80 mM | 0.0318 mL | 0.1588 mL | 0.3175 mL | 0.7938 mL | |
| 100 mM | 0.0254 mL | 0.1270 mL | 0.2540 mL | 0.6350 mL |
SP-alkyne Related Classifications
HY-161389 Related Classifications
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