Carboplatin

Alias: JM-8; NSC-241240; JM8; NSC241240; JM 8; NSC 241240; CBDCA; Carboplatin Hexal; Carboplatino; US trade names: Paraplat; Paraplatin; Foreign brand names: Blastocarb; Carboplat; Carbosin; Carbosol; Carbotec; Displata; Ercar; Nealorin; Novoplatinum; Paraplatin AQ; Paraplatine; Platinwas; Ribocarbo
Cat No.:V1425 Purity: ≥98%
Carboplatin (formerly known as JM-8, CBDCA, NSC-241240; Paraplat; Paraplatin; Blastocarb; Carboplat; Carbosin; Carbosol; Carbotec; Displata; Ercar) is an approved anticancer drug that acts as a DNA synthesis inhibitor by binding to DNA (DNA alkylator) and interfering with the cell's repair mechanism in cancer cells.
Carboplatin Chemical Structure CAS No.: 41575-94-4
Product category: DNA(RNA) Synthesis
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Carboplatin (formerly known as JM-8, CBDCA, NSC-241240; Paraplat; Paraplatin; Blastocarb; Carboplat; Carbosin; Carbosol; Carbotec; Displata; Ercar) is an approved anticancer drug that acts as a DNA synthesis inhibitor by binding to DNA (DNA alkylator) and interfering with the cell's repair mechanism in cancer cells. It is used to treat a few types of cancer, primarily head, neck, and ovarian cancers. It undergoes intracellular activation to generate reactive platinum complexes that attach to nucleophilic sites in DNA, including GC-rich regions, to create DNA-protein cross-links as well as intrastrand and interstrand cross-links. These effects of carboplatin on DNA and proteins lead to cell growth inhibition and apoptosis.

Biological Activity I Assay Protocols (From Reference)
Targets
DNA Alkylator
ln Vitro

In vitro activity: Carboplatin shows a suppressive effect on the growth of cells in a panel of human ovarian cancer cell lines, SKOV3, IGROV-1, and A2780 cells, with IC50 values of 2.2 μM, 12.4 μM, and 6.1 μM, respectively.[1] Additionally, lung carcinoid cell lines such as UMC-11, H727, and H835 cells demonstrate the anti-proliferative activities of carboplatin, with IC50 values of 36.4 μM, 3.4 μM, and 35.8 μM, respectively.[2]

ln Vivo
Carboplatin (60 mg/kg intraperitoneally) administered as a single agent in A2780 tumor xenografts exhibits a moderate antitumor effect, with day 6 tumor weights (T/C) of 67% and relative tumor volumes of 8.4 versus 11.9 on that day.[1] In comparison to the vehicle group, carboplatin treatment causes a 42% reduction in tumor mass and delays the growth of the tumor in the VC8 (Brca2-deficient) xenografts.[3]
Cell Assay
3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assays: Ovarian cancer cells bearing the exponential growth markers A2780, SKOV3, IGROV-1, and HX62 are cultured in 96-well plates. To allow for three to four doubling times, a range of drug concentrations are added, and the plates are then incubated for 72 hours. Every experiment is run in three duplicates. Assays for sulforhodamine B (SRB): A2780 cells that are growing exponentially are plated in 96-well microtitre plates. In studies looking into concurrent exposure, cells are subjected to 96 hours of exposure to escalating concentrations of both medications. Cells are exposed to escalating concentrations of 17-AAG or carboplatin for a duration of 24 hours in order to conduct experiments examining the impact of exposure sequence. In order to give the A2780 cells at least one doubling time (18–24 hours), a 24-hour exposure period to the first agent was selected. The medium is then replaced after the cells are cleaned using sterile phosphate buffered saline. Subsequently, the medium or second medication, which the cells were not exposed to during the first 24 hours, is added and left for 96 hours. Every experiment is run in three duplicates. The well-established principles of the median effect analysis method are applied to the analysis of combination study results. An internal spreadsheet is used to calculate the combination's effects.
Animal Protocol
Mice: In female athymic NCr nude mice (nu/nu), the A2780 human ovarian cancer cell line is cultivated as a subcutaneous xenograft by injecting 4 × 106 cells into each flank. Six mice per group are randomly assigned to receive treatment with either a control vehicle (43% ethanol, 33% polypropylene glycol, and 24% cremaphor diluted 1:7 with sterile water) days 1-4, 80 mg/kg intraperitonially (17-AAG), 60 mg/kg IP day 0 of carboplatin, or a combination of both (17-AAG, 80 mg/kg IP days 1-4) and Carboplatin, 60 mg/kg IP day 0). Tumor growth is measured three times per week, and volumes are computed using the following verified formula: volume = 4.19 × (a/4 + b/4)3, where a represents the longer diameter and b the shorter. Next, tumor volumes are expressed as a percentage of the volume at treatment initiation, or relative tumor volume.
References

[1]. Cancer Chemother Pharmacol . 2008 Oct;62(5):769-78.

[2]. Clin Transl Oncol . 2011 Jan;13(1):43-9.

[3]. Mol Cancer Ther . 2012 Sep;11(9):1948-58.

[4]. Clin Cancer Res . 2004 Mar 1;10(5):1633-44.

[5]. Anticancer Res . 2011 Sep;31(9):2713-22.

[6]. Cancer Res . 2014 Jul 15;74(14):3913-22.

[7]. Br J Cancer. 1995 Dec; 72(6): 1406–1411.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C6H12N2O4PT
Molecular Weight
371.25
Exact Mass
371.04
Elemental Analysis
C, 19.41; H, 3.26; N, 7.55; O, 17.24; Pt, 52.55
CAS #
41575-94-4
Related CAS #
41575-94-4
Appearance
White solid powder
SMILES
C1CC(C1)(C(=O)O)C(=O)O.[NH2-].[NH2-].[Pt+2]
InChi Key
VSRXQHXAPYXROS-UHFFFAOYSA-N
InChi Code
InChI=1S/C6H8O4.2H2N.Pt/c7-4(8)6(5(9)10)2-1-3-6;;;/h1-3H2,(H,7,8)(H,9,10);2*1H2;/q;2*-1;+2
Chemical Name
azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+)
Synonyms
JM-8; NSC-241240; JM8; NSC241240; JM 8; NSC 241240; CBDCA; Carboplatin Hexal; Carboplatino; US trade names: Paraplat; Paraplatin; Foreign brand names: Blastocarb; Carboplat; Carbosin; Carbosol; Carbotec; Displata; Ercar; Nealorin; Novoplatinum; Paraplatin AQ; Paraplatine; Platinwas; Ribocarbo
HS Tariff Code
2931.90.9051
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~14 mg/mL (~37.7 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 10 mg/mL (26.94 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).

Solubility in Formulation 2: Water: 14 mg/mL

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6936 mL 13.4680 mL 26.9360 mL
5 mM 0.5387 mL 2.6936 mL 5.3872 mL
10 mM 0.2694 mL 1.3468 mL 2.6936 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04440358 Active
Recruiting
Device: Exablate BBBD
Drug: Carboplatin
Recurrent Glioblastoma InSightec October 13, 2020 Phase 1
Phase 2
NCT02436993 Active
Recruiting
Drug: Carboplatin
Drug: Paclitaxel
Breast Carcinoma University of California, Irvine April 2015 Phase 2
NCT03414684 Active
Recruiting
Drug: Carboplatin
Drug: Nivolumab
Breast Cancer Dana-Farber Cancer Institute January 30, 2018 Phase 2
NCT02531932 Active
Recruiting
Drug: Carboplatin
Drug: Everolimus
Breast Cancer Amy Tiersten December 16, 2015 Phase 2
NCT02547987 Active
Recruiting
Drug: Docetaxel
Drug: Carboplatin
Breast Cancer Mothaffar Rimawi November 1, 2015 Phase 2
Biological Data
  • Comparison of the effect of DMSO on the biological activity of cisplatin, carboplatin and oxaliplatin. Cancer Res . 2014 Jul 15;74(14):3913-22.
  • Comparison of the effect of DMSO on cisplatin, carboplatin and oxaliplatin-mediated DNA damage and cell death. Cancer Res . 2014 Jul 15;74(14):3913-22.
  • The mTOR inhibitor RAD001 sensitized different breast cancer cell lines to the cytotoxic effect of carboplatin. Anticancer Res . 2011 Sep;31(9):2713-22.
  • The combination of low concentrations of carboplatin and RAD001 resulted in the alteration of cell-cycle related proteins after long-term culture in MCF-7 and BT-474 cell lines. Anticancer Res . 2011 Sep;31(9):2713-22.
  • Effects of dexamethsone (DEX) on antitumor activity of carboplatin and gemcitabine chemotherapy in nude mice bearing human lung cancer A549 or H1299 xenografts. Clin Cancer Res . 2004 Mar 1;10(5):1633-44.
  • In vivo efficacy of ABT-888 in combination with carboplatin in Brca2 isogenic CHO xenograft models. Mol Cancer Ther . 2012 Sep;11(9):1948-58.
  • Cell death of BRCA and BRCA-complemented cell lines after treatment with ABT-888, carboplatin, or ABT-888/carboplatin combination. Mol Cancer Ther . 2012 Sep;11(9):1948-58.
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