RO8994 MedChemExpress (MCE)

Product Name	RO8994
Synonyms	RO8994 CS-2264 RO 8994 RO-8994 (2'S,3R,4'S,5'R)-N-[4-(Aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide Synonyms RO8994 CS-2264 RO 8994 RO-8994 (2'S,3R,4'S,5'R)-N-[4-(Aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide Spiro[3H-indole-3,3'-pyrrolidine]-5'-carboxamide, N-[4-(aminocarbonyl)-2-methoxyphenyl]-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-(2,2-dimethylpropyl)-1,2-dihydro-2-oxo-, (2'S,3R,4'S,5'R)-
CAS	1309684-94-3
EINECS
Chemical Formula	C31H31Cl2FN4O4
Molecular Weight	613.51
inchi
Package	10 mM * 1 mL;5 mg;10 mg;50 mg
Price	Email to quote
Descriptions	RO8994 RO8994 MedChemExpress (MCE) HY-16999 1309684-94-3 99.62% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions RO8994 RO8994 MedChemExpress (MCE) HY-16999 1309684-94-3 99.62% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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. RO8994 dose-dependently and non-genotoxically induces p53 stabilization, cell cycle arrest and Apoptosis in tumor cells retainingwt p53[3]. Activity Results for RO8994 in a Biochemical Binding Assay and Human Cancer Cell Proliferation Assays[1][2][3] compd HTRF IC50 (nM) SJSA IC50 (μM) SW480 IC50 (μM) RO8994 5 0.013 5.19 Antiproliferative Activity of RO8994 in Human Cancer Cell lines[1][2][3] compd MTT IC50 (μM) selectivity RO8994 0.02 312 RO8994 inhibits tumor growth in human SJSA1 tumor xenografts models[3]. Human Liver Microsomal Stability and Mean Single Dose PK Parameters of RO8994 in C57 Male Mice by Oral and IV Dosing[1][2][3] compd HLM_CL (mL/min/kg) PO dose (mg/kg) PO AUC/dose (μg·hr/mL/mg/kg) PO Cmax (μg/mL) IV dose (mg/kg) CL (mL/min/kg) t1/2 (h) F (%) RO8994 7.5 25 3.7 5.8 0.64 5.8 7.1 92 \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief] [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.
Last Update	2025-04-01 14:45:47

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