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Background Information:
NVP-HDM201 (Siremadlin) (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. It is currently in clinical development.
APIM050055: NVP-HDM201 (SIREMADLIN) (HDM-201)
CAS No.: 1448867-41-1.
Molecular Formula: C26H24Cl2N6O4.
Molecular Weight: 555.4 (or refer to Certificate of Analysis, batch specific).
Purity: 99.5% chemical and optical purity (achiral and chiral HPLCs).
QC: Achiral and Chiral HPLCs, NMR and Quantitative Elemental Analysis Report.
Solubility: Refer to certificate of analysis.
Storage: Refer to certificate of analysis.
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