PROTAC XPO1 degrader-1
Based on 1 Customer Validation
PROTAC XPO1 degrader-1 is an XPO1 degrader. PROTAC XPO1 degrader-1 exhibits anti-proliferative effects, can induce cell apoptosis, inhibit NF-κB activity, and cause cell cycle arrest in the G1 phase. PROTAC XPO1 degrader-1 can be used in research on hematological malignancies.
(Pink: CRM1 ligand (HY-170672); Blue: Ligands for E3 Ligase ligand (HY-170671); Black: linker (HY-W010525)).
For research use only. We do not sell to patients.
- Purity: 99.77%
- CAS No.: 3105680-00-7
- Formula: C33H35ClF3N7O7
- Molecular Weight:734.12
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Storage: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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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
PROTAC XPO1 degrader-1 (Compound 2c) effectively degrades XPO1 protein in MV4-11 acute myeloid leukemia (AML) cells with a DC50 of 23.67 nM[1]. PROTAC XPO1 degrader-1 exhibits significant anti-proliferative effects, with IC50 values of 0.142 μM and 0.186 μM against MV4-11 and MOLM-13 cells, respectively[1]. PROTAC XPO1 degrader-1 (100-500 nM; 24 h) effectively induces apoptosis in MV4-11 cells through the caspase pathway[1]. PROTAC XPO1 degrader-1 (100-200 nM; 24 h) can arrest the cell cycle of MV4-11 cells in the G1 phase[1]. PROTAC XPO1 degrader-1 (50 nM; 24 h) reduces cell migration in MV4-11 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV4-11
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Concentration:100, 200, 500 nM
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Incubation Time:24 h
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Result:Induced apoptosis in 71.4 % of the cells at a concentration of 200 nM. Significantly increased the activation of caspase-3/7 in a concentration-dependent manner.
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Cell Line:MV4-11
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Concentration:5, 10, 25, 50, 100 ,500 nM
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Incubation Time:12 h
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Result:Reduced the protein level of XPO1 in cells in a concentration-dependent manner.
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Cell Line:MV4-11
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Concentration:100, 200 nM
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Incubation Time:24 h
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Result:Caused the proportion of cells arrested in the G1 phase to rise from 39.50% to 60.28% as the concentration increased (from 0 to 200 nM).
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Cell Line:MV4-11
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Concentration:50 nM
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Incubation Time:24 h
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Result:Resulted in approximately a 42.6 % reduction in MV4-11 cell migration at 50 nM.
Chemical Information
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CAS No. 3105680-00-7
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Appearance Solid
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Molecular Weight 734.12
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Formula C33H35ClF3N7O7
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Color Off-white to light yellow
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SMILES
ClC1=C(C(F)(F)F)C=CC(NN2C(C(C)=C(CCC(NCC3CCN(C4=CC=C(C(NC5C(NC(CC5)=O)=O)=O)C(OC)=C4)CC3)=O)C2=O)=O)=N1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (136.22 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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)
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 (3.41 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 (3.41 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 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.
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.
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
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 | 1.3622 mL | 6.8109 mL | 13.6218 mL | 34.0544 mL |
| 5 mM | 0.2724 mL | 1.3622 mL | 2.7244 mL | 6.8109 mL | |
| 10 mM | 0.1362 mL | 0.6811 mL | 1.3622 mL | 3.4054 mL | |
| 15 mM | 0.0908 mL | 0.4541 mL | 0.9081 mL | 2.2703 mL | |
| 20 mM | 0.0681 mL | 0.3405 mL | 0.6811 mL | 1.7027 mL | |
| 25 mM | 0.0545 mL | 0.2724 mL | 0.5449 mL | 1.3622 mL | |
| 30 mM | 0.0454 mL | 0.2270 mL | 0.4541 mL | 1.1351 mL | |
| 40 mM | 0.0341 mL | 0.1703 mL | 0.3405 mL | 0.8514 mL | |
| 50 mM | 0.0272 mL | 0.1362 mL | 0.2724 mL | 0.6811 mL | |
| 60 mM | 0.0227 mL | 0.1135 mL | 0.2270 mL | 0.5676 mL | |
| 80 mM | 0.0170 mL | 0.0851 mL | 0.1703 mL | 0.4257 mL | |
| 100 mM | 0.0136 mL | 0.0681 mL | 0.1362 mL | 0.3405 mL |
PROTAC XPO1 degrader-1 Related Classifications
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