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Background Information:
RG7388 (Idasanutlin) is the second generation inhibitor of P53-MDM2 interaction. It is orally active, potently and selectively antagonizing the P53-MDM2 interaction with Ki at low nM. Highly optimized from pyrrolidin-based derivatives, RG7388 represents a distinctive, brand-new structural category of MDM2 ligand, a significant departure from the nutlin-based, first generation ligands exemplified by RG7112. Like RG7112, RG7388 binds selectively to the p53 site on the surface of the MDM2 molecule, effectively displacing p53 from MDM2, leading to p53 stabilization and activation of the p53 pathway. However, RG7388, as compared with its predecessor, binds to the MDM2 protein with a higher potency and selectivity, and has substantially improved pharmacological properties and superior clinical efficacy at lower doses and exposures.
Reference:
1. B. Higgins, et al, Antitumor Activity of the MDM2 Antagonist RG7388, Mol Cancer Ther 2013;12(11 Suppl):B55.
2. Q Ding, et al, Discovery of RG7388, a Potent and Selective p53–MDM2 Inhibitor in Clinical Development, J. Med. Chem., 2013, 56 (14), pp 5979–5983* Sophisticated instrumentation, such as NOESY and COSY, has been involved in reaffirmation of the structure. It is a product with the highest standard in every aspect, manifested by HPLC-MS, Chiral HPLC, NMR, Quantitative Elemental Analysis, and activity assay.
APIM050309: RG7388 (IDASANUTLIN)
CAS No.: 1229705-06-9.
Molecular Formula: C31H29Cl2F2N3O4?0.8H2O.
Molecular Weight: 630.9.
Purity: 99.8-99.9% Pure by achiral and chiral HPLCs.
QC: HPLC-MS, NMR, Chiral HPLC and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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