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 Purity: 98.04% ee.: 100%
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

Size Price Stock Quantity
5 mg USD 580 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2000 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3350 In-stock
Estimated Time of Arrival: December 31
100 mg USD 5600 Get quote
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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.
Clinical Trial
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

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (247.30 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.2365 mL 6.1825 mL 12.3649 mL
5 mM 0.2473 mL 1.2365 mL 2.4730 mL
10 mM 0.1236 mL 0.6182 mL 1.2365 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    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

  • 2.

    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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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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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