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HDM201

Cat. No. M7535
HDM201 Structure
Synonym:

NVP-HDM201

Size Price Availability Quantity
5mg USD 240 In stock
10mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

In vitro: HDM201 binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction of the two proteins and leading to the activation of the p53 pathway. It induces robust p53-dependent cell cycle arrest and apoptosis in human p53 wild-type tumor cells. HDM201 exhibits highly selectivity across a panel of cancer cell lines.

In vivo: HDM201 displays desirable pharmacokinetic and pharmacodynamic profiles in animals together with excellent oral bioavailability. Application of the compound using various dosing schedules triggers rapid and sustained activation of p53-dependent pharmacodynamic biomarkers resulting in tumor regression in multiple xenografted models of p53 wild-type human cancers.

Protocol
Cell Experiment
Cell lines Melanoma cells
Preparation method Melanoma cells were seeded in 96-well plates 24 h before 72 h of treatment with nutlin-3 RG7388, HDM201, GSK2830371 or combinations. The cells were fixed using Carnoy’s fixative followed by Sulforhodamine B (SRB) assay.
Concentrations 0.2 μM
Incubation time 72 h
Animal Experiment
Animal models Mice
Formulation 0.5% methylcellulose and 0.1% Tween 80
Dosages 100 mg/kg
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 555.41
Formula C26H24Cl2N6O4
CAS Number 1448867-41-1
Purity >98%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Targeting negative regulation of p53 by MDM2 and WIP1 as a therapeutic strategy in cutaneous melanoma.
Wu CE, et al. Br J Cancer. 2018 Feb 20;118(4):495-508. PMID: 29235570.

Resistance mechanisms to TP53-MDM2 inhibition identified by in vivo piggyBac transposon mutagenesis screen in an Arf-/- mouse model.
Chapeau EA, et al. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156. PMID: 28265066.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: HDM201, NVP-HDM201 supplier, Mdm2, inhibitors

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