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Satraplatin

Satraplatin is a platinum-based anticancer chemotherapeutic that is used in cisplatin-resistant cancers; like other platinum compounds, it forms DNA adducts and inhibits DNA repair. Satraplatin induces G2/M phase cell cycle arrest, inhibiting the proliferation of oral squamous cell carcinoma cells. Satraplatin also upregulates expression of p21 and cyclin B1 and increases caspase- and Fas-mediated apoptosis in colorectal cancer cells.

References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18971450

Cas No.

129580-63-8

Purity

≥98%

Formula

C10H22Cl2N2O4Pt

Formula Wt.

498.26

Chemical Name

(OC-6-43)-bis(acetato-O)amminedichloro(cyclohexanamine)-platinum

Synonym

Poplat

Appearance

Light yellow crystalline powder

Figg WD, Chau CH, Madan RA, et al. Phase II study of satraplatin and prednisone in patients with metastatic castration-resistant prostate cancer: a pharmacogenetic assessment of outcome and toxicity. Clin Genitourin Cancer. 2013 Sep;11(3):229-37. PMID: 23684781.

Kalimutho M, Minutolo A, Grelli S, et al. Satraplatin (JM-216) mediates G2/M cell cycle arrest and potentiates apoptosis via multiple death pathways in colorectal cancer cells thus overcoming platinum chemo-resistance. Cancer Chemother Pharmacol. 2011 Jun;67(6):1299-312. PMID: 20734047.

Yamano Y, Shiiba M, Negoro K, et al. Antitumor activity of satraplatin in cisplatin-resistant oral squamous cell carcinoma cells. Head Neck. 2011 Mar;33(3):309-17. PMID: 20848452.

Fokkema E, Groen HJ, Helder MN, et al. JM216-, JM118-, and cisplatin-induced cytotoxicity in relation to platinum-DNA adduct formation, glutathione levels and p53 status in human tumour cell lines with different sensitivities to cisplatin. Biochem Pharmacol. 2002 Jun 1;63(11):1989-96. PMID: 12093475.

BGJ-399