RG7388 (IDASANUTLIN)

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.