1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
    Apoptosis
  3. Milademetan tosylate hydrate

Milademetan tosylate hydrate (Synonyms: DS-3032b; DS-3032 tosylate hydrate)

Cat. No.: HY-101266B
Handling Instructions

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.

Milademetan tosylate hydrate Chemical Structure

Milademetan tosylate hydrate Chemical Structure

CAS No. : 2095625-97-9

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Description

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 Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

808.74

Formula

C₃₇H₄₄Cl₂FN₅O₈S

CAS No.

2095625-97-9

SMILES

CC1=CC=C(S(=O)(O)=O)C=C1.O=C2NC3=CC(Cl)=CC=C3[[email protected]]24C5(N[[email protected]]([[email protected]@H]4C6=CC=NC(Cl)=C6F)C(N[[email protected]@H]7CC[[email protected]](OC7)C(N)=O)=O)CCC(C)(CC5)C.[H]O[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Milademetan tosylateDS-3032bDS-3032 tosylateMDM-2/p53E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseAcutemyeloidleukemiasolidtumorAMLneuroblastomaInhibitorinhibitorinhibit

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Milademetan tosylate hydrate
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