Tulmimetostat
Based on 1 Customer Validation
Tulmimetostat (CPI-0209) is an orally active EZH1/EZH2 inhibitor that targets and inhibits the EZH2 enzyme.Tulmimetostat has antitumor activity and is used in a variety of solid tumor studies.
For research use only. We do not sell to patients.
- Purity: 99.45%
- CAS No.: 2567686-02-4
- Formula: C28H36ClN3O5S
- Molecular Weight:562.12
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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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All Histone Methyltransferase Isoforms
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Biological Activity
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EZH2 |
EZH1 |
Tulmimetostat is sensitive to AR-dependent prostate cancer cell lines (including LNCaP, 22Rv1, and VCaP) and AR-dependent cell line-derived transplanted tumor (CDX) and patient-derived transplanted tumor (PDX) models[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2567686-02-4
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Appearance Solid
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Molecular Weight 562.12
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Formula C28H36ClN3O5S
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Color White to off-white
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SMILES
CC1=C2C(O[C@@](O2)([C@]3([H])CC[C@](N4CC(C4)OC)([H])CC3)C)=C(C=C1C(NCC5=C(C=C(NC5=O)C)SC)=O)Cl
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Synonyms
CPI-0209
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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 (177.90 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 (4.45 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 (4.45 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (17.79 mM); Clear solution; Need ultrasonic
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 (272 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
[1]. WHO Drug Information, Vol. 35, No. 4, 2021. Geneva: World Health Organization; 2022.
[3]. Morschhauser F, et al. Taking the EZ way: Targeting enhancer of zeste homolog 2 in B-cell lymphomas. Blood Rev. 2022 Nov;56:100988. [Content Brief]
[4]. Qiu J, et al. The complex role of EZH2 in the tumor microenvironment: opportunities and challenges for immunotherapy combinations. Future Med Chem. 2020 Aug;12(15):1415-1430. [Content Brief]
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 | 1.7790 mL | 8.8949 mL | 17.7898 mL | 44.4745 mL |
| 5 mM | 0.3558 mL | 1.7790 mL | 3.5580 mL | 8.8949 mL | |
| 10 mM | 0.1779 mL | 0.8895 mL | 1.7790 mL | 4.4474 mL | |
| 15 mM | 0.1186 mL | 0.5930 mL | 1.1860 mL | 2.9650 mL | |
| 20 mM | 0.0889 mL | 0.4447 mL | 0.8895 mL | 2.2237 mL | |
| 25 mM | 0.0712 mL | 0.3558 mL | 0.7116 mL | 1.7790 mL | |
| 30 mM | 0.0593 mL | 0.2965 mL | 0.5930 mL | 1.4825 mL | |
| 40 mM | 0.0445 mL | 0.2224 mL | 0.4447 mL | 1.1119 mL | |
| 50 mM | 0.0356 mL | 0.1779 mL | 0.3558 mL | 0.8895 mL | |
| 60 mM | 0.0296 mL | 0.1482 mL | 0.2965 mL | 0.7412 mL | |
| 80 mM | 0.0222 mL | 0.1112 mL | 0.2224 mL | 0.5559 mL | |
| 100 mM | 0.0178 mL | 0.0889 mL | 0.1779 mL | 0.4447 mL |
Tulmimetostat Related Classifications
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