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Merck
CN

SML2811

Phenanthriplatin

>97% (NMR)

别名:

(SP-4-3)-Diamminechlorido(phenanthridine)platinum(II) nitrate, PhenPt, cis-[Pt(NH3)2(phenanthridine)Cl]NO3

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关于此项目

经验公式(希尔记法):
C13H15ClN4O3Pt
化学文摘社编号:
分子量:
505.81
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
>97% (NMR)
Form:
powder
Quality level:
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Quality Level

assay

>97% (NMR)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

Cl[Pt](N)([N+]1=C2C=CC=CC2=C3C=CC=CC3=C1)N.[O-][N+]([O-])=O

InChI key

BELJCNWNXQVJPZ-UHFFFAOYSA-M

Biochem/physiol Actions

Cationic monofunctional DNA-binding platinum (II) complex with significantly greater anticancer activity than cisplatin, oxaliplatin, and pyriplatin.
Phenanthriplatin is a cationic monofunctional DNA-binding platinum (II) complex with significantly greater anticancer activity (IC50 in μM = 0.035/Ntera2, 0.22/A549, 0.30/HeLa, 0.59/U2OS, 0.74/PC3, 0.94/MCF7, 2.02/HT29; 72 h, MTT assay) than cisplatin, oxaliplatin, and pyriplatin. Enhanced cellular uptake due to its hydrophobic phenanthridine ligand as well as more rapid DNA covalent-binding activity both contribute to its superior anticancer efficacy. Phenanthriplatin binds more effectively to 5′-deoxyguanosine monophosphate than to N-acetyl methionine, whereas pyriplatin reacts equally to both.


存储类别

11 - Combustible Solids

wgk

WGK 3



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Amit A Vernekar et al.
Journal of the American Chemical Society, 140(12), 4279-4287 (2018-03-20)
Efficient loading of drugs in novel delivery agents has the potential to substantially improve therapy by targeting the diseased tissue while avoiding unwanted side effects. Here we report the first systematic study of the loading mechanism of phenanthriplatin and its
Matthew W Kellinger et al.
Journal of the American Chemical Society, 135(35), 13054-13061 (2013-08-10)
Transcription inhibition by platinum anticancer drugs is an important component of their mechanism of action. Phenanthriplatin, a cisplatin derivative containing phenanthridine in place of one of the chloride ligands, forms highly potent monofunctional adducts on DNA having a structure and
Daniele Veclani et al.
Journal of the American Chemical Society, 140(43), 14024-14027 (2018-09-07)
The monofunctional platinum drug phenanthriplatin (phenPt) blocks the replication of cancer cells even if it reacts with only one guanine base. However, there is still insufficient experimental data to improve its cytotoxicity and all previously proposed chemical modifications of the



全球贸易项目编号

货号GTIN
SML2811-5MG04061842182664
SML2811-25MG04061842182657