
HDM-201
CAS No. 1448867-41-1
HDM-201( NVP-HDM 201 | NVP HDM201 | Siremadlin )
Catalog No. M11927 CAS No. 1448867-41-1
HDM-201 (NVP-HDM 201, Siremadlin)?is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM.
Purity : >98% (HPLC)






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25MG | 326 | In Stock |
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Biological Information
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Product NameHDM-201
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NoteResearch use only, not for human use.
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Brief DescriptionHDM-201 (NVP-HDM 201, Siremadlin)?is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM.
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DescriptionHDM-201 (NVP-HDM 201, Siremadlin)?is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM; a second generation p53-MDM2 inhibitor that recently entered phase I clinical trial.
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In VitroSiremadlin (NVP-HDM201) disrupts both human and murine TP53- MDM2 interactions, with nanomolar cellular IC50 values, blocking TP53 degradation.
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In VivoSiremadlin (NVP-HDM201) is an imidazolopyrrolidinone analogue, showing a very advantageous in vivo profile. NVP-HDM201 has recently entered Phase 1 clinical trials in cancer patients. Constitutive PB mutagenesis in Arf?/? mice provides a collection of spontaneous tumors with characterized insertional genetic landscapes. Tumors are allografted in large cohorts of mice to assess the pharmacologic effects of Siremadlin (NVP-HDM201). Sixteen out of 21 allograft models are sensitive to Siremadlin (NVP-HDM201) but ultimately relapse under treatment. A comparison of tumors with acquired resistance to Siremadlin (NVP-HDM201) and untreated tumors identified 87 genes that are differentially and significantly targeted by the PB transposon. Siremadlin (NVP-HDM201) administered either daily at a low dose or once at a high dose revealed a differentiated engagement of the p53 molecular response. In contrast to the daily low dose treatment regimen, the single high dose Siremadlin (NVP-HDM201) regimen results in a rapid and dramatic induction of p53-dependent PUMA expression and apoptosis. This is consistent with the finding that a single high dose Siremadlin (NVP-HDM201) treatment, administered orally or intravenously, results in a robust and sustained tumor regression. Overall, both daily and once every 3 weeks dosing regimen shows comparable long term efficacy in preclinical studies. The ongoing clinical trial is currently designed to compare both dosing regimens with regard to efficacy and tolerability.
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SynonymsNVP-HDM 201 | NVP HDM201 | Siremadlin
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PathwayApoptosis
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TargetMDM2-p53
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RecptorMDM2-p53
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Research Area——
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Indication——
Chemical Information
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CAS Number1448867-41-1
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Formula Weight555.4125
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Molecular FormulaC26H24Cl2N6O4
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Purity>98% (HPLC)
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SolubilityDMSO : ≥ 56.75 mg/mL 102.18 mM
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SMILESO=C1N(C2=CC(Cl)=CN(C)C2=O)[C@@H](C3=CC=C(Cl)C=C3)C4=C1N=C(C5=CN=C(OC)N=C5OC)N4C(C)C
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Chemical Name(S)-5-(5-chloro-1-methyl-2-oxo-1,2-dihydropyridin-3-yl)-6-(4-chlorophenyl)-2-(2,4-dimethoxypyrimidin-5-yl)-1-isopropyl-5,6-dihydropyrrolo[3,4-d]imidazol-4(1H)-one
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Furet P, et al. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4837-41.
2. Chapeau EA, et al. Proc Natl Acad Sci U S A. 2017 Mar 21;114(12):3151-3156.
molnova catalog



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HDM-201
HDM-201 (NVP-HDM 201, Siremadlin)?is a highly potent p53-MDM2 interaction inhibitor with biochemical IC50 of 0.13 nM, cellular IC50 of 90 nM.