| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2095625-97-9 | [Synonyms]
Milademetan tosylate
Milademetan (tosylate hydrate) | [Molecular Formula]
C37H42Cl2FN5O7S | [MOL File]
2095625-97-9.mol | [Molecular Weight]
790.73 |
| Chemical Properties | Back Directory | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 200 mg/mL (247.30 mM; Need ultrasonic) | [form ]
Solid | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53[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.
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| [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.
[4] Viktor Arnhold, et al. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. ncotarget. 2018 Jan 5; 9(2): 2304–2319. DOI:10.18632/oncotarget.23409 |
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