1309684-94-3
Chemical Structure
RO8994
- CAS No.: 1309684-94-3
- Formula:C31H31Cl2FN4O4
- Molecular Weight:613.51
IUPAC Name: (2'S,3R,4'S,5'R)-N-(4-carbamoyl-2-methoxyphenyl)-6-chloro-4'-(3-chloro-2-fluorophenyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide
InChIKey: MURAVORBGFDSMA-ISKXDESKSA-N
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
Biological Activity: 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].
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RO8994 | 99.70% | 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. | ||||||||||||||||||||
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- [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.
Keywords
