Transplatin
* Please be kindly noted products are not for therapeutic use. We do not sell to patients.
| Category | Bioactive by-products |
| Catalog number | BBF-03990 |
| CAS | 14913-33-8 |
| Molecular Weight | 300.05 |
| Molecular Formula | Cl2H6N2Pt |
Online Inquiry
Description
The less-active isomer of the DNA damanging, platinum antitumor drug cisplatin. Transplatin is used in the treatment of a variety of solid tumors. Transplatin's anti-tumor activity can be activated by light.
Specification
| Synonyms | Trans-Dichlorodiamineplatinum(II); Azane; Cisplatin |
| IUPAC Name | azane;dichloroplatinum |
| Canonical SMILES | N.N.Cl[Pt]Cl |
| InChI | InChI=1S/2ClH.2H3N.Pt/h2*1H;2*1H3;/q;;;;+2/p-2 |
| InChI Key | LXZZYRPGZAFOLE-UHFFFAOYSA-L |
Properties
| Antibiotic Activity Spectrum | neoplastics (Tumor) |
Reference Reading
1.Enhanced kinetic stability of [Pd2L4]4+ cages through ligand substitution.
Preston D1, McNeill SM2, Lewis JE1, Giles GI2, Crowley JD1. Dalton Trans. 2016 Apr 14. [Epub ahead of print]
There is considerable interest in exploiting metallosupramolecular cages as drug delivery vectors. Recently, we developed a [Pd2L4]4+ cage capable of binding two molecules of cisplatin. Unfortunately, this first generation cage was rapidly decomposed by common biologically relevant nucleophiles. In an effort to improve the kinetic stability of these cage architectures here we report the synthesis of two amino substituted tripyridyl 2,6-bis(pyridin-3-ylethynyl)pyridine () ligands (with amino groups either in the 2-() or 3-() positions of the terminal pyridines) and their respective [Pd2()4]4+ cages. These systems have been characterised by 1H, 13C and DOSY NMR spectroscopies, high resolution electrospray mass spectrometry, elemental analysis and, in one case, by X-ray crystallography. It was established, using model palladium(ii) N-heterocyclic carbene (NHC) probe complexes, that the amino substituted compounds were stronger donor ligands than the parent system ( > > ).
2.Four Cu(ii) complexes based on antitumor chelators: synthesis, structure, DNA binding/damage, HSA interaction and enhanced cytotoxicity.
Liu YH1, Li A1, Shao J1, Xie CZ1, Song XQ1, Bao WG1, Xu JY1. Dalton Trans. 2016 Apr 13. [Epub ahead of print]
Four novel copper(ii) complexes [CuII(Bp4mT)(μ-Cl)]2 (), [CuII(μ-Bp4mT)Br]2 (), [CuII(HBpT)Cl] (), and [CuII(HBpT)Br] () (Bp4mT = 2-benzoylpyridine-4-methylthiosemicarbazone, HBpT = 2-benzoylpyridine thiosemicarbazone), were synthesized and characterized using single-crystal X-ray diffraction, elemental analysis, infrared, and ultraviolet-visible spectroscopy. X-ray analysis revealed that complexes and based on the Bp4mT ligand presented dimeric structures in which the Cu(ii) ions were located in a five-coordinated distorted square-pyramidal geometry, whereas both and complexes were mononuclear with the Cu(ii) ions exhibiting a tetracoordinated square planar configuration. Their interactions with calf thymus DNA (CT-DNA) were investigated using viscosity measurements and fluorescence spectroscopy. Multispectroscopic evidence has shown interactions between these complexes and human serum albumin (HSA). All these complexes have exhibited efficient oxidative cleavage of supercoiled DNA in the presence of hydrogen peroxide, presumably via an oxidative mechanism.
3.3D-RISM-MP2 Approach to Hydration Structure of Pt(II) and Pd(II) Complexes: Unusual H-Ahead Mode vs Usual O-Ahead One.
Aono S1, Mori T2,3, Sakaki S1. J Chem Theory Comput. 2016 Mar 8;12(3):1189-206. doi: 10.1021/acs.jctc.5b01137. Epub 2016 Feb 26.
Solvation of transition metal complexes with water has been one of the fundamental topics in physical and coordination chemistry. In particular, Pt(II) complexes have recently attracted considerable interest for their relation to anticancer activity in cisplatin and its analogues, yet the interaction of the water molecule and the metal center has been obscured. The challenge from a theoretical perspective remains that both the microscopic solvation effect and the dynamical electron correlation (DEC) effect have to be treated simultaneously in a reasonable manner. In this work we derive the analytical gradient for the three-dimensional reference interaction site model Møller-Plesset second order (3D-RISM-MP2) free energy. On the basis of the three-regions 3D-RISM self-consistent field (SCF) method recently proposed by us, we apply a new layer of the Z-vector method to the CP-RISM equation as well as point-charge approximation to the derivatives with respect to the density matrix elements in the RISM-CPHF equation to remarkably reduce the computational cost.
4.Galactose conjugated platinum(II) complex targeting the Warburg effect for treatment of non-small cell lung cancer and colon cancer.
Wu M1, Li H2, Liu R1, Gao X1, Zhang M1, Liu P1, Fu Z3, Yang J4, Zhang-Negrerie D5, Gao Q6. Eur J Med Chem. 2016 Mar 3;110:32-42. doi: 10.1016/j.ejmech.2016.01.016. Epub 2016 Jan 14.
Malignant neoplasms exhibit a higher rate of glycolysis than normal cells; this is known as the Warburg effect. To target it, a galactose-conjugated (trans-R,R-cyclohexane-1,2-diamine)-2-chloromalonato-platinum(II) complex (Gal-Pt) was designed, synthesized, and evaluated in five human cancer cell lines and against two different xenograft tumour models. Gal-Pt exhibits much higher aqueous solubility (over 25 times) and improved cytotoxicity than oxaliplatin, especially in human colon (HT29) and lung (H460) cancer cell lines. The safety profile of Gal-Pt was investigated in vivo by exploring the maximum tolerated dose (MTD) and animal mortality rate. The ratios of the animal lethal dosage values to the cytotoxicity in HT29 (LD50/IC50) showed that Gal-Pt was associated with an increased therapeutic index by over 30-fold compared to cisplatin and oxaliplatin. We evaluated in vivo antitumor activity by single agent intravenous treatment comparison studies of Gal-Pt (50 mg/kg as 65% MTD) and cisplatin (3 mg/kg, as 80% MTD) in a H460 lung cancer xenograft model, and with oxaliplatin (7 mg/kg, as 90% MTD) in a HT29 colon cancer xenograft model.
Recommended Products
| BBF-01825 | Loganin | Inquiry |
| BBF-05862 | Epirubicin | Inquiry |
| BBF-03755 | Actinomycin D | Inquiry |
| BBF-02642 | Lactonamycin | Inquiry |
| BBF-03754 | CASTANOSPERMINE | Inquiry |
| BBF-03753 | Baicalin | Inquiry |
Bio Calculators
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
* Total Molecular Weight:
g/mol
Tip: Chemical formula is case sensitive. C22H30N4O √ c22h30n40 ╳
