| Field | Specification |
|---|---|
| Alternative names | DS-3032b; DS-3032 tosylate hydrate |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C37H44Cl2FN5O8S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Milademetan tosylate hydrate, also known as DS-3032 tosylate hydrate or DS-3032b, is a specific, orally active MDM2 inhibitor used in research on acute myeloid leukemia (AML) and solid tumors. It induces G1 cell cycle arrest, senescence and apoptosis[1][2]. It is supplied as a white to off-white solid (C37H44Cl2FN5O8S, MW 808.74) at 98.89% purity.
Physical & Chemical Properties
| CAS Number | 2095625-97-9 |
|---|---|
| Molecular Formula | C37H44Cl2FN5O8S |
| Molecular Weight | 808.74 g/mol |
| Purity | 98.89% |
| Appearance | Solid |
| Color | White to off-white |
| 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] |
| Signaling Pathway | Apoptosis; Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 50 mg/mL (61.82 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| 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). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. ARYL SULFONOHYDRAZIDES. WO 2017069289 A1.
[2]. M.M. Gounder, et al. Milademetan, an oral MDM2 inhibitor, in well-differentiated/dedifferentiated liposarcoma: results from a phase 1 study in patients with solid tumors or lymphomas. European Journal of Cancer 138S2 (2020) S1–S62.
[3]. Li, Yangbing, et al. Development of novel PROTAC Small-Molecule Degraders of MDM2 Protein and Peptidomimetic Inhibitors Targeting WDR5-MLL1 Protein-Protein Interaction.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 50 mg/mL (61.82 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture and light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 5 mg/mL (6.18 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | 5 mg/mL (6.18 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 5 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (6.18 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In neuroblastoma cells carrying wild-type TP53, Milademetan (DS-3032) can stabilize TP53 and selectively induce expression of CDKNA1, BAX and MDM2[3]. Treatment with Milademetan (DS-3032b) increases TP53 target gene expression and brings on G1 cell cycle arrest, senescence and apoptosis[3]. Selective inhibition of viability, proliferation and migration occurs in neuroblastoma cells with wildtype TP53 when they are exposed to Milademetan (DS-3032b, 0-2000 nM), regardless of MYCN status[4].
Cell Viability Assay[4]
| Cell Line | SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines. |
|---|---|
| Concentration | 0-2000 nM. |
| Incubation Time | 24-72 h. |
| 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). |
In Vivo
In mice xenografted with neuroblastoma cells carrying functional TP53, Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival[4].
| Animal Model | SH-SY5Y xenograft tumors in nude mice[4]. |
|---|---|
| Dosage | 50 mg/kg. |
| 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). |
| Result | Survival in the mouse cohort was significantly prolonged. Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Engineered extrachromosomal oncogene amplifications promote tumorigenesis. Nature 2025 Jan;637(8047):955-964. PMID: 39695225
Targeted degradation of MDM2 overcomes feedback regulation of p53 signaling in Merkel cell carcinoma models. J Clin Invest 2026 Jul 1;136(13):e199049. PMID: 42383359
Pharmacological Inhibition of MDM2 Induces Apoptosis in p53-Mutated Triple-Negative Breast Cancer. Int J Mol Sci 2025 Jan 26;26(3):1078. PMID: 39940844
High-Throughput Drug Library Screening in Primary KMT2A-Rearranged Infant ALL Cells Favors the Identification of Drug Candidates That Activate P53 Signaling. Biomedicines 2022 Mar 10;10(3):638. PMID: 35327440
A framework for target discovery in rare cancers. bioRxiv 2024 Nov 20:2024.10.24.620074. PMID: 39484513
Immortalization and transformation of primary cells mediated by engineered ecDNAs. bioRxiv 2023 Jun 26:2023.06.25.546239. PMID: 37425909
