SML2811
Phenanthriplatin
>97% (NMR)
Sinônimo(s):
(SP-4-3)-Diamminechlorido(phenanthridine)platinum(II) nitrate, PhenPt, cis-[Pt(NH3)2(phenanthridine)Cl]NO3
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Selecione um tamanho
5 MG
R$ 818,00
25 MG
R$ 3.295,00
Sobre este item
Fórmula empírica (Notação de Hill):
C13H15ClN4O3Pt
Número CAS:
Peso molecular:
505.81
Código UNSPSC:
12352200
NACRES:
NA.77
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Estamos aqui para ajudarNível de qualidade
Ensaio
>97% (NMR)
Formulário
powder
cor
white to beige
solubilidade
DMSO: 2 mg/mL, clear
temperatura de armazenamento
2-8°C
cadeia de caracteres SMILES
Cl[Pt](N)([N+]1=C2C=CC=CC2=C3C=CC=CC3=C1)N.[O-][N+]([O-])=O
chave InChI
BELJCNWNXQVJPZ-UHFFFAOYSA-M
1 of 4
Este Item | SML2556 | SML1062 | SML2298 |
|---|---|---|---|
| assay >97% (NMR) | assay >97% (NMR) | assay ≥98% (HPLC) | assay ≥97% (HPLC) |
| form powder | form powder | form powder | form powder |
| Quality Level 100 | Quality Level - | Quality Level 100 | Quality Level - |
| storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C |
| solubility DMSO: 2 mg/mL, clear | solubility DMSO: 0.2 mg/mL (warmed) | solubility DMSO: 20 mg/mL, clear | solubility DMSO: 2 mg/mL, clear |
| color white to beige | color faint yellow to dark orange | color white to brown | color white to beige |
Ações bioquímicas/fisiológicas
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.
Código de classe de armazenamento
11 - Combustible Solids
Classe de risco de água (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
Jerry D Monroe et al.
PloS one, 13(3), e0192505-e0192505 (2018-03-08)
Unlike cisplatin, which forms bifunctional DNA adducts, monofunctional platinum(II) complexes bind only one strand of DNA and might target cancer without causing auditory side-effects associated with cisplatin treatment. We synthesized the monofunctional triamine-ligated platinum(II) complexes, Pt(diethylenetriamine)Cl, [Pt(dien)Cl]+, and Pt(N,N-diethyldiethylenetriamine)Cl, [Pt(Et2dien)Cl]+
Ga Young Park et al.
Proceedings of the National Academy of Sciences of the United States of America, 109(30), 11987-11992 (2012-07-10)
Monofunctional platinum(II) complexes of general formula cis-[Pt(NH(3))(2)(N-heterocycle)Cl]Cl bind DNA at a single site, inducing little distortion in the double helix. Despite this behavior, these compounds display significant antitumor properties, with a different spectrum of activity than that of classic bifunctional
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