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Carboplatin DNA Synthesis inhibitor

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

제품 번호S1215

CDDP의 유도체인 Carboplatin은 DNA에 결합하여 복제와 전사를 억제하고 세포 사멸을 유도하며 A2780, SKOV-3, IGROV-1 및 HX62 세포에서 세포의 복구 메커니즘을 방해하는 DNA synthesis inhibitor입니다. 이는 DNA 가닥 간 교차결합 및 DNA-단백질 교차결합 형성을 유도합니다. 용액은 불안정하므로 신선하게 준비해야 합니다. DMSO는 백금 기반 약물을 용해하는 데 권장되지 않으며, 이는 쉽게 약물 비활성화를 초래할 수 있습니다.

Carboplatin Antineoplastic and Immunosuppressive Antibiotics 억제제 Chemical Structure

화학 구조

분자량: 371.25

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품질 관리

배치: 순도: 99.98%

99.98

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

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	제형	활성 설명	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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	371.25	화학식	C₆H₁₂N₂O₄Pt	보관 (수령일로부터)	2 years 4°C/3 years -20°C(in the dark) powder
CAS 번호	41575-94-4	SDF 다운로드		원액 보관	용액은 불안정합니다. 신선하게 준비하거나 소량의 사전 포장된 크기를 구매하십시오. 수령 즉시 재포장하십시오.
동의어	NSC 241240, JM-8, CBDCA			Smiles	C1CC(C1)(C(=O)O)C(=O)O.[NH2-].[NH2-].[Pt+2]

용해도

In vitro
배치:

Water : 4.5 mg/mL

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

특징	This product is not recommended to be dissolved in dimethylsulfoxide (DMSO).
Targets/IC₅₀/Ki	DNA synthesis (A2780, SKOV-3, IGROV-1, HX62 cells)
시험관 내(In vitro)	Carboplatin은 인간 난소암 세포주 패널(A2780, SKOV3, IGROV-1 세포 포함)에서 각각 6.1 μM, 12.4 μM, 2.2 μM의 IC50 값으로 세포 증식에 억제 효과를 보입니다. 이 화합물은 또한 폐 유암종 세포주인 UMC-11, H727, H835 세포에서 각각 36.4 μM, 3.4 μM, 35.8 μM의 IC50 값으로 항증식 활성을 나타냅니다.
생체 내(In vivo)	A2780 종양 이종이식 모델에서 Carboplatin (60 mg/kg i.p. 투여) 단일 요법은 6일째 상대적 종양 부피가 대조군 11.9에 비해 8.4로, 6일째 종양 무게가 대조군 대비 (T/C) 67%로 완만한 항종양 효과를 보였습니다. VC8 (Brca2 결핍) 이종이식 모델에서 이 화합물 처리는 종양 성장을 지연시키고 대조군에 비해 종양 질량을 42% 감소시켰습니다.
참조	[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/

적용 분야

방법	바이오마커	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

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
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

기술 지원

취급 설명서

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자주 묻는 질문

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

답변:
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.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):