For research use only. Not for therapeutic Use.
CGM097 (Cat No.:I001200) is a selective small molecule inhibitor of the MDM2-p53 interaction, a critical pathway involved in tumor suppression. By disrupting the interaction between MDM2 and the p53 tumor suppressor protein, CGM097 reactivates p53, which can trigger cell cycle arrest and apoptosis in cancer cells. This mechanism is particularly useful in cancers where p53 function is impaired by overactive MDM2. CGM097 is being studied in clinical trials for its potential to treat various cancers, especially those with p53 mutations.
| Catalog Number | I001200 |
| CAS Number | 1313363-54-0 |
| Synonyms | (S)-1-(4-chlorophenyl)-7-isopropoxy-6-methoxy-2-(4-(methyl(((1r,4S)-4-(4-methyl-3-oxopiperazin-1-yl)cyclohexyl)methyl)amino)phenyl)-1,2-dihydroisoquinolin-3(4H)-one |
| Molecular Formula | C₃₈H₄₇ClN₄O₄ |
| Purity | ≥95% |
| Target | Metabolic Enzyme/Protease |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| InChI | InChI=1S/C38H47ClN4O4/c1-25(2)47-35-22-33-28(20-34(35)46-5)21-36(44)43(38(33)27-8-10-29(39)11-9-27)32-16-14-30(15-17-32)41(4)23-26-6-12-31(13-7-26)42-19-18-40(3)37(45)24-42/h8-11,14-17,20,22,25-26,31,38H,6-7,12-13,18-19,21,23-24H2,1-5H3/t26?,31?,38-/m0/s1 |
| InChIKey | CLRSLRWKONPSRQ-CPOWQTMSSA-N |
| SMILES | CC(C)OC1=C(C=C2CC(=O)N(C(C2=C1)C3=CC=C(C=C3)Cl)C4=CC=C(C=C4)N(C)CC5CCC(CC5)N6CCN(C(=O)C6)C)OC |
| Reference | </br>1:The HDM2 (MDM2) Inhibitor NVP-CGM097 Inhibits Tumor cell Proliferation and Shows Additive Effects with 5-Fluorouracil on the p53 – p21 – Rb – E2F1 Cascade in the p53wildtype Neuroendocrine Tumor Cell Line GOT1. Reuther C, Heinzle V, Nölting S, Herterich S, Hahner S, Halilovic E, Jeay S, Wuerthner JU, Aristizabal Prada ET, Spöttl G, Maurer J, Auernhammer CJ.Neuroendocrinology. 2016 Nov 21. [Epub ahead of print] No abstract available. PMID: 27871087 </br>2:Correction: A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097. Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.Elife. 2016 Nov 17;5. pii: e19317. doi: 10.7554/eLife.19317. No abstract available. PMID: 27852439 Free PMC Article</br>3:Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors. Holzer P, Masuya K, Furet P, Kallen J, Valat-Stachyra T, Ferretti S, Berghausen J, Bouisset-Leonard M, Buschmann N, Pissot-Soldermann C, Rynn C, Ruetz S, Stutz S, Chène P, Jeay S, Gessier F.J Med Chem. 2015 Aug 27;58(16):6348-58. doi: 10.1021/acs.jmedchem.5b00810. Epub 2015 Aug 5. PMID: 26181851 </br>4:A distinct p53 target gene set predicts for response to the selective p53-HDM2 inhibitor NVP-CGM097. Jeay S, Gaulis S, Ferretti S, Bitter H, Ito M, Valat T, Murakami M, Ruetz S, Guthy DA, Rynn C, Jensen MR, Wiesmann M, Kallen J, Furet P, Gessier F, Holzer P, Masuya K, Würthner J, Halilovic E, Hofmann F, Sellers WR, Graus Porta D.Elife. 2015 May 12;4. doi: 10.7554/eLife.06498. Erratum in: Elife. 2016 Nov 17;5:. PMID: 25965177 Free PMC Article |
