Cisplatin

Antitumor agent



ALX-400-040-M050	50 mg	40.00 USD

ALX-400-040-M250	250 mg	104.00 USD

Replaces Prod. #: BML-GR356

A potent platinum-based antineoplastic drug. Its mode of action invovles formation of inter- and intrastrand DNA adducts which activate signaling pathways culminating in apoptosis. Platinated DNA adducts also enhance poisoning of DNA topoisomerase I. Cisplatin synergizes with a variety of anticancer agents. Tumor cells rapidly develop resistance to cisplatin and numerous agents are available to block or reverse resistance.

Product Specification

Alternative Name:	cis-Platinum(ll)diamine dichloride

Endotoxin Content:	≤1.0EU/mg

Formula:	Cl₂H₆N₂Pt

MW:	300.0

Purity:	≥98% (Assay)

Appearance:	Off-white to orange powder.

CAS:	15663-27-1

MI:	14: 2317

RTECS:	TP2450000

Solubility:	Soluble in dimethyl formamide (16mg/ml) or DMSO (10mg/ml); sparingly soluble in water; insoluble in 100% ethanol.

Long Term Storage:	+20°C

Hazard:	TOXIC.

Handling:	Protect from light.

Background / Technical Information:	In aqueous solution cis-trans isomerization of cisplatin occurs. Isomerization is increased at elevated temperatures. Stability of cisplatin in aqueous solutions was enhanced by increasing the sodium chloride (NaCl) concentration to 0.9% and was adversely affected in alkaline solutions such as sodium bicarbonate solutions. Further, even though soluble in DMSO we do not recommend to dissolve cisplatin in DMSO. The DMSO inserts itself into the ligand. It is recommended to prepare all solutions fresh and protect from light.

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Product Literature References

Paclitaxel encapsulated in cationic liposomes increases tumor microvessel leakiness and improves therapeutic efficacy in combination with Cisplatin: S. Strieth et al.; Clin. Cancer. Res. 14, 4603 (2008), Abstract;

Protein kinase C inhibitor Go6976 augments caffeine-induced reversal of chemoresistance to cis-diamminedichloroplatinum-II (CDDP) in a human ovarian cancer model: L. Qamar et al.; Gynecol. Oncol. 110, 425 (2008), Abstract;

Effectiveness of hsp90 inhibitors as anti-cancer drugs: L. Xiao, et al.; Mini Rev. Med. Chem. 6, 1137 (2006), (Review), Abstract;

Platinated DNA adducts enhance poisoning of DNA topoisomerase I by camptothecin: R.C. van Waardenburg et al.; J. Biol. Chem. 279, 54502 (2004), Abstract;

Cisplatin: mode of cytotoxic action and molecular basis of resistance: Z.H. Siddik ; Oncogene 22, 7265 (2003), Abstract;

Biomolecular targets for platinum antitumor drugs: R.N. Bose ; Mini Rev. Med. Chem. 2, 103 (2002), Abstract;

Cisplatin (CDDP) specifically induces apoptosis via sequential activation of caspase-8, -3 and -6 in osteosarcoma: K. Seki, et al.; Cancer Chemother. Pharmacol. 45, 199 (2000), Abstract;

Cisplatin-induced apoptosis in human proximal tubular epithelial cells is associated with the activation of the Fas/Fas ligand system: M.S. Razzaque, et al.; Histochem. Cell Biol. 111, 359 (1999), Abstract;

Mitochondrial changes during the apoptotic process of HeLa cells exposed to cisplatin: J. Melendez-Zajgla, et al.; Biochem. Mol. Biol. Int. 47, 765 (1999), Abstract;

The tyrosine kinase c-Abl regulates p73 in apoptotic response to cisplatin-induced DNA damage: J.G. Gong, et al.; Nature 399, 806 (1999), Abstract;

Cisplatin induces a persistent activation of JNK that is related to cell death: I. Sanchez-Perez, et al.; Oncogene 16, 533 (1998), Abstract;

Telomere loss in cells treated with cisplatin: T. Ishibashi & S.J. Lippard; PNAS 95, 4219 (1998), Abstract;