PROTAC SMARCA2 degrader-8
Based on 1 Customer Validation
PROTAC SMARCA2 degrader-8 is a SMARCA2 PROTAC degrader with a DC50 of 28 nM in A375 cells. PROTAC SMARCA2 degrader-8 forms a crystallizable ternary complex with the SMARCA4 bromodomain and VBC, promoting the ubiquitination and proteasomal degradation of SMARCA2. PROTAC SMARCA2 degrader-8 can be used in melanoma research.
(Pink: Target protein ligand; Blue: VHL ligand (HY-112078); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.54%
- CAS No.: 2669027-50-1
- Formula: C43H50N10O5S
- Molecular Weight:818.99
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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
Biological Activity
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SMARCA2 |
PROTAC SMARCA2 degrader-8 (Compound 1) (100 nM; 60 s contact time, 300 s dissociation time) forms a negatively cooperative ternary complex with purified VBC and SMARCA2BD, with a ternary binding affinity of 4.7 nM and a cooperativity factor of 12.8[1].
PROTAC SMARCA2 degrader-8 (dose-gradient dilution; 2 h treatment) induces SMARCA2 degradation in A375 cells, with a DC50 of 28 nM and a maximum degradation rate of 98%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2669027-50-1
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Appearance Solid
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Molecular Weight 818.99
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Formula C43H50N10O5S
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Color White to off-white
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SMILES
O=C(N[C@@H](C(C)(C)C)C(N1[C@H](C(N[C@H](C2=CC=C(C3=C(C)N=CS3)C=C2)C)=O)C[C@@H](O)C1)=O)C4=CC=NC(N5CCN(C6=CC(C7=CC=CC=C7O)=NN=C6N)CC5)=C4
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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 (122.10 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 (3.05 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 (3.05 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 (275 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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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 | 1.2210 mL | 6.1051 mL | 12.2102 mL | 30.5254 mL |
| 5 mM | 0.2442 mL | 1.2210 mL | 2.4420 mL | 6.1051 mL | |
| 10 mM | 0.1221 mL | 0.6105 mL | 1.2210 mL | 3.0525 mL | |
| 15 mM | 0.0814 mL | 0.4070 mL | 0.8140 mL | 2.0350 mL | |
| 20 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 25 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2210 mL | |
| 30 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0175 mL | |
| 40 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7631 mL | |
| 50 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 mL | |
| 60 mM | 0.0204 mL | 0.1018 mL | 0.2035 mL | 0.5088 mL | |
| 80 mM | 0.0153 mL | 0.0763 mL | 0.1526 mL | 0.3816 mL | |
| 100 mM | 0.0122 mL | 0.0611 mL | 0.1221 mL | 0.3053 mL |
PROTAC SMARCA2 degrader-8 Related Classifications
HY-161882 Related Classifications
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