HDM201 (Siremadlin)

For research use only.

Catalog No.S8606 Synonyms: NVP-HDM201

HDM201 (Siremadlin) Chemical Structure

Molecular Weight(MW): 555.41

HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.

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Biological Activity

Description HDM201 is a novel, highly potent and selective inhibitor of the p53-Mdm2 interaction with affinity constant for Mdm2 in the picomolar range and a selectivity ratio greater than 10000-fold vs Mdm4.
Targets
p53/MDM2 interaction [1]
()
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[1]. 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[2].

Assay
Methods Test Index PMID
Western blot
DUSP6 / p53 / p-p53 / MDM2 / p21 ; 

PubMed: 30577494     


Immunoblotting of WM35 after siRNA knockdown of DUSP6 for 24 h followed by treatment with 1 µM HDM201 for 6 and 24 h. 

30577494
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[2].

Protocol

Solubility (25°C)

In vitro DMSO 100 mg/mL (180.04 mM)
Ethanol 3 mg/mL (5.4 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 555.41
Formula

C26H24Cl2N6O4

CAS No. 1448867-41-1
Storage powder
in solvent
Synonyms NVP-HDM201

In vivo Formulation Calculator (Clear solution)

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03940352 Recruiting Drug: HDM201|Biological: MBG453|Drug: Venetoclax Acute Myeloid Leukemia (AML)|High-risk Myelodysplastic Syndrome (MDS) Novartis Pharmaceuticals|Novartis June 24 2019 Phase 1
NCT02601378 Active not recruiting Drug: LXS196|Drug: LXS196 and HDM201 Uveal Melanoma Novartis Pharmaceuticals|Novartis February 1 2016 Phase 1
NCT02343172 Completed Drug: HDM201|Drug: LEE011 Liposarcoma Novartis Pharmaceuticals|Novartis March 13 2015 Phase 1|Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID