PeptideDB

Carboplatin

CAS: 41575-94-4 F: C6H12N2O4Pt W: 371.25

Carboplatin (NSC 241240) is a DNA synthesis inhibitor which binds to DNA, inhibits replication and transcription and ind
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Bioactivity 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 CDDP and a potent anti-cancer agent.
Target DNA Alkylator
Invitro 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].
Name Carboplatin
CAS 41575-94-4
Formula C6H12N2O4Pt
Molar Mass 371.25
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Reference [1]. Natarajan G, et al. Increased DNA-binding activity of cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts: activation theory revisited. Biochem Pharmaco [2]. Banerji U, et al. An in vitro and in vivo study of the combination of the heat shock protein inhibitor 17-allylamino-17-demethoxygeldanamycin and carboplatin in human ovarian cancer models. Cancer Chemother Pharmacol. 2008 Oct;62(5):769-78. [3]. Clark CC, et al. Enhancement of synthetic lethality via combinations of ABT-888, a PARP inhibitor, and carboplatin in vitro and in vivo using BRCA1 and BRCA2 isogenic models. Mol Cancer Ther. 2012 Sep;11(9):1948-58. [4]. Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116. [5]. Hall MD, Telma KA, Chang KE, et al. Say no to DMSO: dimethylsulfoxide inactivates cisplatin, carboplatin, and other platinum complexes. Cancer Res. 2014;74(14):3913-3922.