DOT1L808
Based on 1 Customer Validation
DOT1L808 is a potent and highly selective DOT1L PROTAC degrader with a DC50 value of 5 nM. DOT1L808 can promote the ubiquitination and degradation of DOT1L. DOT1L808 exhibits antitumor activity in an orthotopic leukemia model.
(Pink: DOT1L ligand (HY-181790); Blue: VHL ligand (HY-181791); Black: linker).
For research use only. We do not sell to patients.
- Purity: 98.31%
- Formula: C61H72ClF3N14O9S2
- Molecular Weight:1301.89
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Storage:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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VHL |
DOT1L 5 nM (DC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice (female, 6-8 weeks old, tail vein injection of 1.5 × 106 MV-4−11-Luc cells)[1]
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Dosage:25 mg/kg
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Administration:i.p.; twice daily; 2 weeks (5 days per week)
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Result:Markedly reduced bioluminescent signal (total photon flux per second) relative to vehicle-treated mice, indicating significant inhibition of disseminated leukemia growth.
Showed no significant body weight changes compared to vehicle controls.
Chemical Information
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Appearance Solid
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Molecular Weight 1301.89
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Formula C61H72ClF3N14O9S2
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Color White to off-white
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SMILES
CC1=C(SC=N1)C2=CC=C(C(OCCN3CCN(CC3)CCN4CCN(CC4)C5=NC=NC(NC6=C(C=CC(S(C)(=O)=O)=C6)N[C@H](C7=C(C=CC=N7)Cl)C8=C9OC(F)(OC9=CC=C8)F)=N5)=C2)CNC([C@@H]%10C[C@H](CN%10C([C@H](C(C)(C)C)NC(C%11(CC%11)F)=O)=O)O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (76.81 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 (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 (1.92 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 (1.92 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 (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 (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 | 0.7681 mL | 3.8406 mL | 7.6811 mL | 19.2029 mL |
| 5 mM | 0.1536 mL | 0.7681 mL | 1.5362 mL | 3.8406 mL | |
| 10 mM | 0.0768 mL | 0.3841 mL | 0.7681 mL | 1.9203 mL | |
| 15 mM | 0.0512 mL | 0.2560 mL | 0.5121 mL | 1.2802 mL | |
| 20 mM | 0.0384 mL | 0.1920 mL | 0.3841 mL | 0.9601 mL | |
| 25 mM | 0.0307 mL | 0.1536 mL | 0.3072 mL | 0.7681 mL | |
| 30 mM | 0.0256 mL | 0.1280 mL | 0.2560 mL | 0.6401 mL | |
| 40 mM | 0.0192 mL | 0.0960 mL | 0.1920 mL | 0.4801 mL | |
| 50 mM | 0.0154 mL | 0.0768 mL | 0.1536 mL | 0.3841 mL | |
| 60 mM | 0.0128 mL | 0.0640 mL | 0.1280 mL | 0.3200 mL |
DOT1L808 Related Classifications
HY-181789 Related Classifications
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