Milademetan tosylate hydrate
Based on 5 publication(s) in Google Scholar
Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
For research use only. We do not sell to patients.
- Purity: 98.89%
- CAS No.: 2095625-97-9
- Formula: C37H44Cl2FN5O8S
- Molecular Weight:808.74
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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
Publications Citing Use of MedChemExpress (MCE) Milademetan tosylate hydrate
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Biological Activity
Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53[3].
Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis[3].
Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines.
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Concentration:0-2000 nM.
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Incubation Time:24-72 h.
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Result:Reduced viability in a dose- and time-dependent manner.
Exhibited IC50 values of 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM in SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines, respectively (72 h).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SH-SY5Y xenograft tumors in nude mice[4].
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Dosage:50 mg/kg.
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Administration:Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
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Result:Survival in the mouse cohort was significantly prolonged.
Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.
Chemical Information
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CAS No. 2095625-97-9
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Appearance Solid
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Molecular Weight 808.74
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Formula C37H44Cl2FN5O8S
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Color White to off-white
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SMILES
CC1=CC=C(S(=O)(O)=O)C=C1.O=C2NC3=CC(Cl)=CC=C3[C@]24C5(N[C@H]([C@@H]4C6=CC=NC(Cl)=C6F)C(N[C@@H]7CC[C@H](OC7)C(N)=O)=O)CCC(C)(CC5)C.[H]O[H]
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Synonyms
DS-3032b; DS-3032 tosylate hydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (5)
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Journal Impact Factor
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Most Recent
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Nature
2025 Jan;637(8047):955-964. PMID: 39695225 -
Int J Mol Sci
Pharmacological Inhibition of MDM2 Induces Apoptosis in p53-Mutated Triple-Negative Breast Cancer. [Abstract]2025 Jan 26;26(3):1078. PMID: 39940844 -
Biomedicines
High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling. [Abstract]2022 Mar 10;10(3):638. PMID: 35327440 -
bioRxiv
2024 Nov 20:2024.10.24.620074. PMID: 39484513 -
bioRxiv
2023 Jun 26:2023.06.25.546239. PMID: 37425909
Solvent & Solubility
DMSO : 50 mg/mL (61.82 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (sealed storage, away from moisture and 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 (287 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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 (sealed storage, away from moisture and 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 | 1.2365 mL | 6.1825 mL | 12.3649 mL | 30.9123 mL |
| 5 mM | 0.2473 mL | 1.2365 mL | 2.4730 mL | 6.1825 mL | |
| 10 mM | 0.1236 mL | 0.6182 mL | 1.2365 mL | 3.0912 mL | |
| 15 mM | 0.0824 mL | 0.4122 mL | 0.8243 mL | 2.0608 mL | |
| 20 mM | 0.0618 mL | 0.3091 mL | 0.6182 mL | 1.5456 mL | |
| 25 mM | 0.0495 mL | 0.2473 mL | 0.4946 mL | 1.2365 mL | |
| 30 mM | 0.0412 mL | 0.2061 mL | 0.4122 mL | 1.0304 mL | |
| 40 mM | 0.0309 mL | 0.1546 mL | 0.3091 mL | 0.7728 mL | |
| 50 mM | 0.0247 mL | 0.1236 mL | 0.2473 mL | 0.6182 mL | |
| 60 mM | 0.0206 mL | 0.1030 mL | 0.2061 mL | 0.5152 mL |
Milademetan tosylate hydrate Related Classifications
HY-101266B Related Classifications
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