MS8709
Based on 1 Customer Validation
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP PROTAC degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.87%
- CAS No.: 3060730-06-2
- Formula: C64H95F2N11O7S
- Molecular Weight:1200.57
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | GI50 |
4.1 μM
Compound: 10; MS8709
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Cytotoxicity against human 22Rv1 cells assessed as growth inhibition measured for 7 days
Cytotoxicity against human 22Rv1 cells assessed as growth inhibition measured for 7 days
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[PMID: 38602846] |
| K562 | GI50 |
2 μM
Compound: 10; MS8709
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Cytotoxicity against human K562 cells assessed as growth inhibition incubated for 7 days
Cytotoxicity against human K562 cells assessed as growth inhibition incubated for 7 days
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[PMID: 38602846] |
| K562 | IC50 |
2 μM
Compound: 10; MS8709
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Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 8 days
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 8 days
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[PMID: 38602846] |
| NCI-H1299 | GI50 |
5 μM
Compound: 10; MS8709
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Cytotoxicity against human NCI-H1299 cells assessed as growth inhibition incubated for 8 days
Cytotoxicity against human NCI-H1299 cells assessed as growth inhibition incubated for 8 days
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[PMID: 38602846] |
MS8709 (compound 10) induces significant degradation of G9a and GLP at both 0.3 and 3 µM. MS8709 (with an 11-carbon linker) induces more than 70% of G9a and around 50% of GLP degradation at 0.3 µM and complete degradation for both proteins at 3 µM[1].
MS8709 (10, 1 μM, 24 h) induces G9a/GLP degradation in a VHL- and UPS-dependent manner[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. 3060730-06-2
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Appearance Solid
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Molecular Weight 1200.57
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Formula C64H95F2N11O7S
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Color White to off-white
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SMILES
O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCCNC(CCCN2CCC(NC3=C4C=C(OC)C(OCCCN5CCCC5)=CC4=NC(N6CCC(F)(F)CC6)=N3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (41.65 mM; ultrasonic and warming and heat to 60°C; 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 (protect from light). 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 (protect from light). 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 (2.08 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 (2.08 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (269 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)
- 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 (protect from light). 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 | 0.8329 mL | 4.1647 mL | 8.3294 mL | 20.8234 mL |
| 5 mM | 0.1666 mL | 0.8329 mL | 1.6659 mL | 4.1647 mL | |
| 10 mM | 0.0833 mL | 0.4165 mL | 0.8329 mL | 2.0823 mL | |
| 15 mM | 0.0555 mL | 0.2776 mL | 0.5553 mL | 1.3882 mL | |
| 20 mM | 0.0416 mL | 0.2082 mL | 0.4165 mL | 1.0412 mL | |
| 25 mM | 0.0333 mL | 0.1666 mL | 0.3332 mL | 0.8329 mL | |
| 30 mM | 0.0278 mL | 0.1388 mL | 0.2776 mL | 0.6941 mL | |
| 40 mM | 0.0208 mL | 0.1041 mL | 0.2082 mL | 0.5206 mL |
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