Carboplatin

Description

Description

Carboplatin is a DNA synthesis inhibitor by binding to DNA and interfering with the cell’s repair mechanism.

In vitro

Carboplatin exhibits an inhibitory effect on cell proliferation in a human ovarian cancer cell line panel, including A2780, SKOV3, and IGROV-1 cells with IC50 of 6.1 μM, 12.4 μM and 2.2 μM, respectively. ^[1] Carboplatin also show the anti-proliferative activities in lung carcinoid cell line, such as UMC-11, H727, and H835 cells with IC50 of 36.4 μM, 3.4 μM and 35.8 μM, respectively. ^[2]

In A2780 tumor xenografts, Carboplatin (60 mg/kg via i.p.) given as single agents shows a modest antitumor effect with the relative tumor volumes on day 6 of 8.4 compared to the control of 11.9, and the day 6 tumor weights relative to control (T/C) of 67%. ^[1] For the VC8 (Brca2-deficient) xenografts, Carboplatin treatment delays tumor growth and reduces tumor mass by 42% compared to the vehicle group. ^[3]

A DNA synthesis inhibitor.

Carboplatin

Catalog No.S1215

Carboplatin is a DNA synthesis inhibitor by binding to DNA and interfering with the cell’s repair mechanism.

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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw

Cell lines	A2780, SKOV3, IGROV-1 and HX62
Concentrations	0-200 μM
Incubation Time	72 hours
Method	3-(4,5-dimethylthiazol-2yl)-2,5-diphenyltetrazolium bromide (MTT) assays: Exponentially growing A2780, SKOV3, IGROV-1 and HX62 ovarian cancer cells are plated in 96 well plates. A range of drug concentrations are added and the plates are incubated for 72 hours to allow for 3–4 doubling times. Each experiment is carried out in triplicate. Sulforhodamine B (SRB) assays: Exponentially growing A2780 cells are plated in 96 well microtitre plates. For experiments studying concomitant exposure, cells are exposed to increasing concentrations of both drugs for 96 hours. For experiments studying the effect of sequence of exposure to 17-AAG or carboplatin cells are exposed to increasing concentrations of 17-AAG or carboplatin for 24 hours. A period of 24-hour exposure to the first agent is chosen so that the A2780 cells would be exposed to the first drug for at least one doubling time (18-24 hours). The cells are then washed with sterile phosphate buffered saline and the medium is replenished. Following this, the second drug (to which the cells are not exposed to in the first 24 hours) or medium is added for 96 hours. All experiments are carried out in triplicate. The results of combination studies are analyzed using the well-established principles of median effect analysis method. The effects of the combination are calculated using an in-house spreadsheet.

Animal Models	The A2780 human ovarian cancer cell line is grown as a subcutaneous xenograft in female athymic NCr nude mice (nu/nu) in each flank.
Dosages	≤60 mg/kg
Administration	Administered via i.p.
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 5 mg/mL

NCT Number	Recruitment	Conditions	Sponsor /Collaborators	Start Date	Phases
NCT01690468	Not yet recruiting	Ovarian Cancer	H. Lee Moffitt Cancer Center and Research Institute\|Department of Defense\|Cahaba Pharmaceuticals	2014-01	Phase 1\|Phase 2
NCT02016209	Not yet recruiting	Non Small Cell Lung Cancer	Zhejiang University	2014-01	Phase 2
NCT01993810	Not yet recruiting	Stage IIA Non-small Cell Lung Cancer\|Stage IIB Non-small Cell Lung Cancer\|Stage IIIA Non-small Cell Lung Cancer\|Stage IIIB Non-small Cell Lung Cancer	Radiation Therapy Oncology Group\|National Cancer Institute (NCI)	2014-02	Phase 3
NCT01969578	Not yet recruiting	Salivary Gland Cancer	European Organisation for Research and Treatment of Cancer - EORTC	2014-03	Phase 2
NCT01451853	Not yet recruiting	Lung Cancer\|Head and Neck Cancer\|Hearing Loss\|Ototoxicity\|Tinnitus\|Neuropathy	Sound Pharmaceuticals, Incorporated\|VA Puget Sound Health Care System	2014-03	Phase 2

Solubility (25°C) *	In vitro	DMSO	<1 mg/mL (<1 mM)
		Water	<1 mg/mL (<1 mM)
		Ethanol	<1 mg/mL (<1 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol,	5 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name

Click to enlarge	Rating
	Source	PLoS ONE 8(9): e72637. Carboplatin purchased from Selleck
	Method	microscope imaging
	Cell Lines	A1847 cells
	Concentrations	1-200 uM
	Incubation Time	3 days
	Results	The percentage of apoptotic cells increased in epimorphin-treated cells with increasing concentrations of carboplatin