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Carboplatin DNA Synthesis inhibitor

Name: Carboplatin
Brand: Selleck Chemicals
SKU: S1215
Rating: 5 (157 reviews)

Cat.nr.S1215

Carboplatin, een derivaat van CDDP, is een DNA synthesis inhibitor die bindt aan DNA, replicatie en transcriptie remt en celdood induceert en interfereert met het celreparatiemechanisme in A2780, SKOV-3, IGROV-1 en HX62 cellen. Het induceert de vorming van DNA interstrand crosslinks en DNA-eiwit crosslinks. Oplossingen zijn onstabiel en moeten vers worden bereid. DMSO wordt niet aanbevolen om op platina gebaseerde geneesmiddelen op te lossen, wat gemakkelijk kan leiden tot inactivering van het geneesmiddel.

Carboplatin Antineoplastic and Immunosuppressive Antibiotics remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 371.25

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Kwaliteitscontrole

Batch: Zuiverheid: 99.98%

99.98

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
Overig Antineoplastic and Immunosuppressive Antibiotics Inhibitoren	Staurosporine (STS) Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine

Celkweek, behandeling & werkzame concentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
Tca8113/ut	Growth Inhibition Assay	2-25 μM	72 h		inhibits cell viability dose dependently	26137105
Tca8113/CBP	Growth Inhibition Assay	2-25 μM	72 h		inhibits cell viability dose dependently	26137105
Tca8113/PYM	Growth Inhibition Assay	2-25 μM	72 h		inhibits cell viability dose dependently	26137105
SKOV3	Growth Inhibition Assay	60 mg/ml	1-5 d		inhibits cell viability time dependently	26137043
SKOV3	Growth Inhibition Assay	0-4 μg/ml	24/48/72 h		inhibits cell viability dose and time dependently	26125273
SKOV3	Apoptosis Assay	2 μg/ml	48 h		induces apoptosis	26125273
OSA	Clonogenic Assay	2.5/5 μM			results in lower colony formation as compared to either BMI1 siRNA treatment	26110620
A549	Fuction Assay	0/25/50 μM	24 h		downregulates miR-205 expression	25917317
H1975	Fuction Assay	0/25/50 μM	24 h		downregulates miR-205 expression	25917317
A549	Fuction Assay	0/25/50 μM	24 h		upregulates miR-218 expression	25917317
H1975	Fuction Assay	0/25/50 μM	24 h		upregulates miR-218 expression	25917317
A549	Growth Inhibition Assay	25 μM	24 h		inhibits cell growth	25917317
H1975	Growth Inhibition Assay	25 μM	24 h		inhibits cell growth	25917317
MDA-MB-231	Growth Inhibition Assay	0-220 μg/ml	72 h		IC50 = 86 μM	25837691
T47D	Growth Inhibition Assay	0-220 μg/ml	72 h		IC50 = 48.9 μM	25837691
LCTCC	Growth Inhibition Assay				IC50=3.8 µM	25773167
MCTCC	Growth Inhibition Assay				IC50=2.8 µM	25773167
MegTCC	Growth Inhibition Assay				IC50=4.1 µM	25773167
MonoTCC	Growth Inhibition Assay				IC50=5.6 µM	25773167
MCF7	Growth Inhibition Assay	20 μM	72 h		induces cell death of HP1β-depleted MCF7 cells	25769025
A-549	Growth Inhibition Assay	0.5 μM	24 h	DMSO	inhibits cell growth significantly	25755690
A-549	Apoptosis Assay	0.5 μM	48 h	DMSO	shows early apoptosis features including blebbing and chromatin condensation	25755690
A-549	Fuction Assay	0.5 μM	48 h	DMSO	shows aberrant microtubule disruption	25755690
A-549	Fuction Assay	0.5 μM	48 h	DMSO	inhibits of cell migration	25755690
RMG-1	Growth Inhibition Assay				IC50=28.8 ± 3.6 mg/L	25726913
FN-RMG-1	Growth Inhibition Assay				IC50=40.5 ± 4.2 mg/L μM	25726913
RMG-1-hFUT	Growth Inhibition Assay				IC50=58.1 ± 2.4 mg/L	25726913
FN-RMG-1-hFUT	Growth Inhibition Assay				IC50=118.8 ± 13.8 mg/L	25726913
CHP-134	Growth Inhibition Assay	1 μM		DMSO	inhibits significant cell growth combined with GSK2830371	25658463
IMR-32	Growth Inhibition Assay	1 μM		DMSO	inhibits significant cell growth combined with GSK2830371	25658463
CHP-134	Fuction Assay	10 μM		DMSO	induces apoptosis significantly combined with GSK2830371	25658463
IMR-32	Fuction Assay	10 μM		DMSO	induces apoptosis significantly combined with GSK2830371	25658463
A549	Growth Inhibition Assay	0.2-4000 μM	72 h		IC50=126 ± 5.0 μM	25625243
A549/CDDP	Growth Inhibition Assay	0.2-4000 μM	72 h		IC50=240 ± 45.7 μM	25625243
H460	Growth Inhibition Assay		24 h	DMSO	IC50=7.9 μM	25599995
H460	Growth Inhibition Assay	7.9 μM	24 h	DMSO	shows a radiosensitizing effect to X-rays	25599995
NRK-52E	Growth Inhibition Assay		72 h		IC50=100 ± 12.9 μM	25565603
RGE	Growth Inhibition Assay		72 h		IC50=22 ± 7.4 μM	25565603
NRK-52E	Growth Inhibition Assay		72 h		IC80=179 ± 9.5 μM	25565603
RGE	Growth Inhibition Assay		72 h		IC80=63 ± 7.4 μM	25565603
SK-OV-3	Growth Inhibition Assay		72 h		IC50=104.8 μM	25520132
ES-2	Growth Inhibition Assay		72 h		IC50=14.6 μM	25520132
OVCAR-8	Growth Inhibition Assay		72 h		IC50=96.0 μM	25520132
3AO	Growth Inhibition Assay		72 h		IC50=63.4 μM	25520132
A2780	Growth Inhibition Assay		72 h		IC50=145.7 μM	25520132
SW626	Growth Inhibition Assay		72 h		IC50=97.0 μM	25520132
OVCAR-3	Growth Inhibition Assay		72 h		IC50=32.6 μM	25520132
A549	Growth Inhibition Assay				IC50=151.56 ± 53.06 μM	25277461
4T1	Growth Inhibition Assay				IC50=84.62 ± 30.05 μM μM	25277461
BALB/3T3	Growth Inhibition Assay				IC50=14.30 ± 6.68 μM	25277461
B16	Growth Inhibition Assay				IC50=64.30 ± 6.81 μM	25277461
DU 145	Growth Inhibition Assay				IC50=35.04 ± 17.54 μM	25277461
FaDu	Growth Inhibition Assay				IC50=45.39 ± 11.50 μM	25277461
HCV-29T	Growth Inhibition Assay				IC50=48.57 ± 22.49 μM	25277461
HL-60	Growth Inhibition Assay				IC50=11.10 ± 4.47 μM	25277461
HT-29	Growth Inhibition Assay				IC50=89.16 ± 18.86 μM	25277461
H146	Growth Inhibition Assay				IC50=49.6±13.1 μM	25124282
H187	Growth Inhibition Assay				IC50=12.7±2.7 μM	25124282
H128	Growth Inhibition Assay				IC50=106.4±9.6 μM	25124282
H69	Growth Inhibition Assay				IC50=76.9±27.8 μM	25124282
H209	Growth Inhibition Assay				IC50=258.1±99.8 μM	25124282
DMS153	Growth Inhibition Assay				IC50=57.8±9.2 μM	25124282
H526	Growth Inhibition Assay				IC50=7.2±1.7 μM	25124282
DMS114	Growth Inhibition Assay				IC50=85.8±12.8 μM	25124282
DMS53	Growth Inhibition Assay				IC50=146.2±36.4 μM	25124282
HeLa	Growth Inhibition Assay	5-80 μM			inhibits cell growth dose dependently	25109360
MCF-7	Growth Inhibition Assay	5-80 μM			inhibits cell growth dose dependently	25109360
MDA-MB-231	Growth Inhibition Assay	5-80 μM			inhibits cell growth dose dependently	25109360
CaOV3	Growth Inhibition Assay		72 h		IC50=86.1 μM	25068849
OVCAR-3	Growth Inhibition Assay		72 h		IC50=179.5 μM	25068849
OVCAR-5	Growth Inhibition Assay		72 h		IC50=75.7 μM	25068849
SKOV-3	Growth Inhibition Assay		72 h		IC50=504 μM	25068849
OVCAR-4	Growth Inhibition Assay		72 h		IC50=290.6 μM	25068849
OVCAR-8	Growth Inhibition Assay		72 h		IC50=690.2 μM	25068849
MA148	Growth Inhibition Assay		24 h		IC50=83.6 ± 1.4 μg/ml	24831091
A549	Growth Inhibition Assay		24 h		IC50=776.0 ± 1.9 μg/ml	24831091
MDA-MB-231	Growth Inhibition Assay		24 h		IC50=748.0 ± 1.1 μg/ml	24831091
NCI-ADR/RES	Growth Inhibition Assay		24 h		IC50=1753.0 ± 4.4 μg/ml	24831091
MA148	Growth Inhibition Assay		48 h		IC50=28.1 ± 1.0 μg/ml	24831091
A549	Growth Inhibition Assay		48 h		IC50=118.0 ± 1.2 μg/ml	24831091
MDA-MB-231	Growth Inhibition Assay		48 h		IC50=183.0 ± 1.2 μg/ml	24831091
NCI-ADR/RES	Growth Inhibition Assay		48 h		IC50=193.0 ± 1.9 μg/ml	24831091
MA148	Growth Inhibition Assay		72 h		IC50=13.7 ± 1.2 μg/ml	24831091
A549	Growth Inhibition Assay		72 h		IC50=64.3 ± 1.1 μg/ml	24831091
MDA-MB-231	Growth Inhibition Assay		72 h		IC50=99.5 ± 1.1 μg/ml	24831091
NCI-ADR/RES	Growth Inhibition Assay		72 h		IC50=37.4 ± 1.7 μg/ml	24831091
A549	Growth Inhibition Assay		72 h	DMSO	IC50=152.409 μM	24721323
NCI-H157	Growth Inhibition Assay		72 h	DMSO	IC50=89.977 μM	24721323
PC9	Growth Inhibition Assay		72 h		GC50=71.6±9.5 µM	24618809
A549	Growth Inhibition Assay		72 h		GC50=136±31.6 µM	24618809
PC9	Apoptosis Assay	100 µM	72 h		induces apoptosis	24618809
A549	Apoptosis Assay	100 µM	72 h		induces apoptosis	24618809
A549	Growth Inhibition Assay		24 h		IC10=1.476 nM	24396437
H1299	Growth Inhibition Assay		24 h		IC10=0.443 nM	24396437
HCC15	Growth Inhibition Assay		24 h		IC10=0.346 nM	24396437
H157	Growth Inhibition Assay		24 h		IC10=0.81 nM	24396437
A2780	Growth Inhibition Assay				IC50=14.0 ± 1.4 μM	24209693
A2780cisR	Growth Inhibition Assay				IC50=48.9 ± 3.9 μM	24209693
A2780ZD0473R	Growth Inhibition Assay				IC50=64.6 ± 3.2 μM	24209693
SKOV-3	Growth Inhibition Assay				IC50=43.4 ± 3.9 μM	24209693
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit

Molecuulgewicht	371.25	Formule	C₆H₁₂N₂O₄Pt	Opslag (vanaf de datum van ontvangst)	2 years 4°C/3 years -20°C(in the dark) powder
CAS-nr.	41575-94-4	SDF downloaden		Opslag van stamoplossingen	Oplossingen zijn instabiel. Bereid ze vers of koop kleine, voorverpakte formaten. Herverpakken na ontvangst.
Synoniemen	NSC 241240, JM-8, CBDCA			Smiles	C1CC(C1)(C(=O)O)C(=O)O.[NH2-].[NH2-].[Pt+2]

Oplosbaarheid

In vitro
Batch:

Water : 4.5 mg/mL

Ethanol : Insoluble

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Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Kenmerken	This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).
Targets/IC₅₀/Ki	DNA synthesis (A2780, SKOV-3, IGROV-1, HX62 cells)
In vitro	Carboplatin vertoont een remmend effect op celproliferatie in een panel van menselijke eierstokkankercellijnen, waaronder A2780, SKOV3 en IGROV-1 cellen met respectievelijk IC50's van 6,1 μM, 12,4 μM en 2,2 μM. Deze verbinding vertoont ook antiproliferatieve activiteiten in longcarcinoïde cellijnen, zoals UMC-11, H727 en H835 cellen met respectievelijk IC50's van 36,4 μM, 3,4 μM en 35,8 μM.
In vivo	In A2780 tumor xenografts toont Carboplatin (60 mg/kg via i.p.), toegediend als enkelvoudige middelen, een bescheiden antitumor effect met relatieve tumorvolumes op dag 6 van 8,4 vergeleken met de controle van 11,9, en de tumorvolumes op dag 6 relatief ten opzichte van controle (T/C) van 67%. Voor de VC8 (Brca2-deficiënte) xenografts vertraagt deze verbinding de tumorgroei en vermindert de tumormassa met 42% vergeleken met de vehikelgroep.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/18193424/ [2] https://pubmed.ncbi.nlm.nih.gov/21239354/ [3] https://pubmed.ncbi.nlm.nih.gov/22778154/ [4] https://pubmed.ncbi.nlm.nih.gov/15014014/ [5] https://pubmed.ncbi.nlm.nih.gov/21868512/ [6] https://pubmed.ncbi.nlm.nih.gov/24812268/ [7] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2034078/

Toepassingen

Methoden	Biomarkers	PMID
Western blot	p-p38 / p38 / Cleaved PARP / PARP p-p53(S15) / p-p53(S46) / p-p53(S392) / p53 pChK-2 / Chk-2	30049957
Immunofluorescence	γH2AX	24348048
Growth inhibition assay	Cell viability	24348048

Informatie over klinische proeven

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT06393816	Not yet recruiting	Large Cell Neuroendocrine Carcinoma of the Lung	Centre Leon Berard\|Groupe Français de Pneumo-Cancérologie	May 2024	Phase 2
NCT06303713	Not yet recruiting	Prostate Cancer\|Metastatic Prostate Cancer\|Metastatic Castration-resistant Prostate Cancer	Dana-Farber Cancer Institute\|Novartis	May 2024	Phase 1
NCT05846789	Recruiting	Metastatic Breast Cancer\|Triple Negative Breast Cancer\|Estrogen-receptor-low Breast Cancer	Kathy Miller\|Genentech Inc.\|Indiana University	May 2024	Phase 2
NCT06288854	Not yet recruiting	Weight Gain	Rajavithi Hospital	April 3 2024	Not Applicable

Technische ondersteuning

Gebruiksaanwijzing

Tel: +1-832-582-8158 Ext:3

Als u nog andere vragen heeft, laat dan een bericht achter.

Veelgestelde vragen

Vraag 1:
Can you advise what solvent to use and the concentration for it for in vitro use?

Antwoord:
DMSO will affect the activity of platinum agents. For in vitro use, according to our experience in dissolving this compound, we didn't find any solvent can dissolve it alone, but it can be dissolved in co-solvent ethanol:water=1:2 at 15 mg/ml. We didn't test the stability of the drug in such vehicle, so it is recommended to prepare the solution just before use.

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