Milademetan

Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis[1][2].

Product Specifications

CAS Number

[1398568-47-2]

Product Name Alternative

DS-3032

UNSPSC

12352005

Target

Apoptosis; E1/E2/E3 Enzyme; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/Milademetan.html

Purity

98.87

Solubility

DMSO : 16.67 mg/mL (ultrasonic)

Smiles

O=C(NC1=CC(Cl)=CC=C21)[C@]32C4(CCC(C)(C)CC4)N[C@@H](C(N[C@@H]5CC[C@@H](C(N)=O)OC5)=O)[C@@H]3C6=CC=NC(Cl)=C6F

Molecular Formula

C30H34Cl2FN5O4

Molecular Weight

618.53

References & Citations

[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.