tcsc1121 Carboplatin

Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and induces cell death. Carboplatin (NSC 241240) is a derivative of cisplatin and a potent anti-cancer agent.

IC50 & Target: DNA Alkylator^[1]

In Vitro: Carboplatin is an antitumor agent, with an increased DNA-binding activity in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts^[1]. Carboplatin is less cytotoxic to human ovarian cells such as A2780, SKOV3, IGROV1 and HX62 than 17-AAG, with IC₅₀s of 6.177, 12.442, 2.233 and 116.068 μM, respectively. Moreover, Carboplatin does not affect HSP90 or change the activity of 17-AAG to inhibit HSP90^[2]. Carboplatin reduces the viability of Brca1 (IC₅₀, 3.4 μM) and Brca2 cells (IC₅₀, 1.9 μM). Carboplatin (25 μM) combined with ABT-888 also shows an apoptotic effect in BRCA1 cells^[3].

In Vivo: Carboplatin (60 mg/kg, i.p.) shows a modest effect on the tumor, but significantly inhibits tumor growth in combination with 17-AAG in mice bearing A2780 human ovarian cancer xenografts^[2]. Carboplatin (25 mg/kg, p.o.) combined with ABT-888 delays tumor growth in Brca2 xenografts^[3].