NVP-HDM201 - Siremadlin | HDM-201

Based on 19 reference(s) in Google Scholar 8 10 19

Axon 3737

CAS [1448867-41-1]

MF C26H24Cl2N6O4
MW 555.41

  • Purity: 99%
  • Optical purity: 99% e.e.
  • Soluble in DMSO

NVP-HDM201

Description

NVP-HDM201 is an orally bioavailable, potent and selective inhibitor of p53-MDM2 interaction, binding to human MDM2 protein with a picomolar Ki value (0.21 nM). Highly selective against MDM4 protein (Ki = 3300 nM, >10000 fold selectivity). It activates p53 and induces robust p53-dependent cell cycle arrest and apoptosis in human p53 wild-type tumor cells. Its activity and selectivity have been tested and confirmed in both in vitro and in vivo. Application of NVP-HDM201 using various dosing schedules triggers rapid and sustained activation of p53-dependent pharmacodynamics biomarkers resulting in tumor regression in multiple xenorgrafted models of p53 wild-type human cancers.

KEYWORDS: NVP-HDM201 | Supplier | MDM2 inhibitor | Siremadlin | HDM-201 | NVP-HDM-201 | NVP-HDM 201 | CT-HDM201 | CAS [1448867-41-1] | p53 | HDM-MDM | Inhibitor | Enzymes

Potent, selective, and orally bioavailable MDM2-p53 inhibitor

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

Source information

Sold in collaboration with Chemietek

Parent CAS No.

[1448867-41-1]

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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