| Description | Phenanthriplatin, also known as cis-[Pt(NH3)2-(phenanthridine)Cl]NO3, is a new drug candidate. It belongs to a family of platinum(II)-based agents which includes cisplatin, oxaliplatin and carboplatin. Phenanthriplatin Acts As a Covalent Poison of Topoisomerase II Cleavage Complexes. Phenanthriplatin exhibits significantly greater activity than cisplatin and oxaliplatin. The cellular uptake of phenanthriplatin is substantially greater than that of cisplatin and pyriplatin because of the hydrophobicity of the phenanthridine ligand. Phenanthriplatin binds more effectively to 5'-deoxyguanosine monophosphate than to N-acetyl methionine, whereas pyriplatin reacts equally well with both reagents. |
| Synonyms | cis-[Pt(NH3)2-(phenanthridine)Cl]NO3 |
| molecular weight | 501.79 |
| Molecular formula | C13H11ClN4O3Pt |
| CAS | 1416900-51-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| References | 1. Bruno PM, Liu Y, Park GY, Murai J, Koch CE, Eisen TJ, Pritchard JR, Pommier Y, Lippard SJ, Hemann MT. A subset of platinum-containing chemotherapeutic agents kills cells by inducing ribosome biogenesis stress. Nat Med. 2017 Apr;23(4):461-471. doi: 10.1038/nm.4291. Epub 2017 Feb 27. PubMed PMID: 28263311; PubMed Central PMCID: PMC5520548. 2. Ravera M, Gabano E, Zanellato I, Perin E, Arrais A, Osella D. Polyanionic Biopolymers for the Delivery of Pt(II) Cationic Antiproliferative Complexes. Bioinorg Chem Appl. 2016;2016:2380540. Epub 2016 Sep 28. PubMed PMID: 27774043; PubMed Central PMCID: PMC5059510. 3. Riddell IA, Agama K, Park GY, Pommier Y, Lippard SJ. Phenanthriplatin Acts As a Covalent Poison of Topoisomerase II Cleavage Complexes. ACS Chem Biol. 2016 Nov 18;11(11):2996-3001. Epub 2016 Oct 6. PubMed PMID: 27648475; PubMed Central PMCID: PMC5248983. 4. Riddell IA, Johnstone TC, Park GY, Lippard SJ. Nucleotide Binding Preference of the Monofunctional Platinum Anticancer-Agent Phenanthriplatin. Chemistry. 2016 May 23;22(22):7574-81. doi: 10.1002/chem.201600236. Epub 2016 Apr 25. PubMed PMID: 27111128; PubMed Central PMCID: PMC4884344. |