RO8994

RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays) . RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model[1][2][3].

Product Specifications

CAS Number

[1309684-94-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; E1/E2/E3 Enzyme; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/RO8994.html

Concentration

10mM

Purity

99.62

Solubility

DMSO : ≥ 45 mg/mL

Smiles

O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)NC5=CC=C(C(N)=O)C=C5OC

Molecular Formula

C31H31Cl2FN4O4

Molecular Weight

613.51

Precautions

H302, H315, H319, H335

References & Citations

[1]Zhang Z, et al. Discovery of potent and selective spiroindolinone MDM2 inhibitor, RO8994, for cancer therapy. Bioorg Med Chem. 2014 Aug 1;22 (15) :4001-4009.|[2]Zhang Z, et al. Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development. ACS Med Chem Lett. 2013 Dec 29;5 (2) :124-7.|[3]Yu B, Liu H M. The development of new spirooxindoles targeting the p53–MDM2 protein-protein interactions for cancer therapy[J]. Targeting Protein-Protein Interactions by Small Molecules, 2018: 213-237.