RO-5963

RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.

Product information

CAS Number: 1416663-77-8

Molecular Weight: 518.90

Formula: C24H21ClF2N4O5

Chemical Name: 2-[(4E)-4-[(6-chloro-7-methyl-1H-indol-3-yl)methylidene]-2, 5-dioxoimidazolidin-1-yl]-2-(3, 4-difluorophenyl)-N-(1, 3-dihydroxypropan-2-yl)acetamide

Smiles: CC1=C(Cl)C=CC2=C1NC=C2/C=C1/NC(=O)N(C(C2=CC(F)=C(F)C=C2)C(=O)NC(CO)CO)C/1=O

InChiKey: ZFYQBPVMECJUBO-FBCYGCLPSA-N

InChi: InChI=1S/C24H21ClF2N4O5/c1-11-16(25)4-3-15-13(8-28-20(11)15)7-19-23(35)31(24(36)30-19)21(22(34)29-14(9-32)10-33)12-2-5-17(26)18(27)6-12/h2-8,14,21,28,32-33H,9-10H2,1H3,(H,29,34)(H,30,36)/b19-7+

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

RO-5963 (10-20 μM; 48 hours) shows much higher apoptotic activity than Nutlin in both MCF7 and ZR75-30 cell lines. RO-5963 (10 μM, 24 hours) effectively activats p53 and elevates p21 and MDM2 levels.

References:

1. Graves B, et al. Activation of the p53 pathway by small-molecule-induced MDM2 and MDMX dimerization. Proc Natl Acad Sci U S A. 2012 Jul 17;109(29):11788-93.

Products are for research use only. Not for human use.