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Mitoxantrone Topoisomerase 억제제

Name: Mitoxantrone
Brand: Selleck Chemicals
SKU: S1889
Rating: 5 (8 reviews)

제품 번호S1889

Mitoxantrone은 HepG2 및 MCF-7/wt 세포에 대해 각각 2.0 μM, 0.42 mM의 IC50을 갖는 II형 Topoisomerase 억제제입니다.

Mitoxantrone Topoisomerase 억제제 Chemical Structure

화학 구조

분자량: 444.48

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품질 관리

배치: 순도: 99.27%

99.27

관련 타겟	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Aurora Kinase
기타 Topoisomerase 억제제	Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan

세포 배양, 처리 및 작업 농도

세포주	분석 유형	배양 시간	활성 설명
L1210 cell	Cytotoxic assay	48 h	Cytotoxic potency required to inhibit L1210 cell growth by 50% after cell drug contact for 48 hrs, IC50=4e-05 μM
human HL60 cells	Cytotoxic assay	48 h	Cytotoxicity against human HL60 cells after 48 hrs by MTT assay, GI50=0.33 nM
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against MDA435/LCC6 cells by ELISA, IC50=0.35 nM
A2780-cell	Growth inhibition assay		Concentration required to inhibit A2780-cell growth by 50%, IC50=0.55 μM
A2780 cell	Cytotoxic assay	96 h	Cytotoxic potency required to inhibit A2780 cell growth by 50% after cell drug contact for 96 hrs, IC50=0.55 nM
G-361 cell	Cytotoxic assay		Cytotoxic potency required to inhibit G-361 cell growth by 50%, IC50=0.65 nM
HL60 human leukemia cell	Cytotoxic assay	72 h	Compound was tested in vitro for cytotoxicity against HL60 human leukemia cell line (72 hr exposure to compound), IC50=0.81 nM
human HL60 cells	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells after 72 hrs by SRB assay, IC50=2.5 nM
human K562 cells	Cytotoxic assay	5 days	Cytotoxicity against human K562 cells after 5 days by XTT assay, IC50=2.6 nM
CH1-cell	Growth inhibition assay		Concentration required to inhibit CH1-cell growth by 50%, IC50=2.65 nM
uterine sarcoma MES-SA cells	Cytotoxic assay		In vitro cytotoxicity against uterine sarcoma MES-SA cells, IC5=3 nM
MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against MES-SA cells by MTT assay after 72 hrs, IC50=3 nM
A549 cells	Function assay		Tested for inhibitory activity against human tumor cell line A549 (a non small, drug resistant cell line that does not produce P-glycoprotein) of lung carcinoma using sulforhodamine B assay, IC50=3 nM
human LoVo cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human LoVo cancer cell line was determined after 144 hr, IC50=3.3 nM
P388 cells	Proliferation assay		Antiproliferative activity against P388 cells by ELISA, IC50=4.3 nM
MCF-7	Growth inhibition assay		In vitro inhibition of tumor cell growth in the human mammary tumor MCF-7 system, IC50=5 nM
murine L1210 sensitive cell line	Function assay		Anti-tumor activity against murine L1210 sensitive cell line by using MTT assay, IC50=5 nM
human Daudi cells	Proliferation assay	72 h	Antiproliferative activity against human Daudi cells after 72 hrs by MTT assay, IC50=5 nM
SKOV-3-cell	Growth inhibition assay		Concentration required to inhibit SKOV-3-cell growth by 50%, IC50=5.3 nM
human cell line DU145	Cytotoxic assay		In vitro Cytotoxic activity of compound in comparison with reference compounds in human cell line DU145, IC50=5.6 nM
human HCT116 cancer cell line	Cytotoxic assay	144 h	Cytotoxicity against human HCT116 cancer cell line was determined after 144 hr, IC50=5.8 nM
OVCAR-3 cell	Function assay		Inhibitory activity against OVCAR-3 cell line, IC50=5.8 nM
human MES-SA cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA cells after 72 hrs by MTT assay, IC50=6 nM
human PC3 cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human PC3 cancer cell line was determined after 144 hr, IC50=7 nM
MDR cell line K562R	Cytotoxic assay	72 h	Compound was tested in vitro for cytotoxicity against MDR cell line K562R (72 hr exposure to compound), IC50=7.06 nM
WiDr cell	Function assay		Activity against human colon carcinoma sensitive WiDr cell line, IC50=8.1 nM
MXF7 breast cell line	Function assay		Antitumor activity against human mammary carcinoma sensitive MXF7 breast cell line, IC50=8.7 nM
HT-29 cell	Cytotoxic assay		In vitro cytotoxicity was tested against human colon adenocarcinoma HT-29 cell line, IC50=0.01 μM
CHO cell line xrs6	Cytotoxic assay		Cytotoxicity against CHO cell line xrs6, IC50=0.01 μM
human HL60 cells	Growth inhibition assay		Growth inhibition of human HL60 cells by Almar blue assay, GI50=0.01 μM
HT-29 cells	Cytotoxic assay		Cytotoxicity is determined as the concentration required to inhibit the growth of human colon adenocarcinoma (HT-29) cell line, IC50=0.01 μM
human Ishikawa cells	Proliferation assay	72 h	Antiproliferative activity against human Ishikawa cells after 72 hrs by MTT assay, IC50=0.01 μM
HEK293 cells	Cytotoxic assay	72 h	Cytotoxicity against HEK293 cells after 72 hrs by MTT assay, IC50=0.01 μM
human MKN45 cancer cell	Cytotoxic assay	144 h	Cytotoxicity against human MKN45 cancer cell line was determined after 144 hr, IC50=0.012 μM
human LoVo cancer cell	Cytotoxic assay	1 h	Cytotoxicity against human LoVo cancer cell line was determined after 1 hr, IC50=0.012 μM
human FM3 cells	Proliferation assay	72 h	Antiproliferative activity against human FM3 cells after 72 hrs by MTT assay, IC50=0.013 μM
human HL60 cells	Cytotoxic assay	48 h	Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.016 μM
SK-BR-3 cells	Function assay		The IC50 value was measured on human breast cancer cell line SK-BR-3, IC50=0.016 μM
human small-cell lung cancer (SCLC)	Cytotoxic assay		Cytotoxicity against human small-cell lung cancer (SCLC), IC50=0.02 μM
human HCT116 cells	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50=0.022 μM
human HCT116 cells	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=0.025 μM
A0375 cells	Function assay		Inhibitory activity against human tumor cell line A0375 melanoma, IC50=0.026 μM
NCI-H460 cells	Cytotoxic assay	48 h	Cytotoxicity against human NCI-H460 cells after 48 hrs by resazurin dye assay, EC50=0.03 μM
CCRF-CEM cells	Cytotoxic assay	48 h	Cytotoxicity against human CCRF-CEM cells assessed as cell viability after 48 hrs by celltiter-blue assay, IC50=0.036 μM
human HeLa cells	Proliferation assay	72 h	Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay, IC50=0.044 μM
human NCI60 cells	Function assay	48 h	Antitumor activity against human NCI60 cells after 48 hrs by SRB assay, GI50=0.04786 μM
UA375 cells	Function assay		Tested for inhibitory activity against human tumor cell line UA375 of melanoma using sulforhodamine B assay, IC50=0.048 μM
HT1080 cells	Function assay		Inhibitory activity against human tumor cell line HT1080, IC50=0.066 μM
human MES-SA/Dx5 cells	Proliferation assay	72 h	Antiproliferative activity against human MES-SA/Dx5 cells after 72 hrs by MTT assay, IC50=0.073 μM
human RKOp27 cells	Proliferation assay	48 h	Antiproliferative activity against human RKOp27 cells after 48 hrs, EC50=0.09 μM
human HeLa cells	Cytotoxic assay	96 h	Cytotoxicity against human HeLa cells expressing telomerase after 96 hrs by MTT assay, IC50=0.1 μM
human SKOV3 cells	Proliferation assay	48 h	Antiproliferative activity against human SKOV3 cells after 48 hrs, EC50=0.12 μM
human NCI-H460 cells	Proliferation assay	48 h	Antiproliferative activity against human NCI-H460 cells after 48 hrs, EC50=0.12 μM
A549 cells	Cytotoxic assay		In vitro cytotoxic activity against human lung A549 cell line ( standard deviation in parenthesis), IC50=0.3 μM
SF268 cells	Proliferation assay	48 h	Antiproliferative activity against human SF268 cells after 48 hrs, EC50=0.32 μM
human KB/HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human KB/HeLa cells after 48 hrs, EC50=0.36 μM
K562 cells	Growth inhibition assay	72 h	Growth inhibition of human K562 cells after 72 hrs by MTS method, IC50=0.42 μM
MDA-MB-231 cells	Proliferation assay		Antiproliferative activity against human MDA-MB-231 cells, IC50=0.96 μM
SF268 cells	Cytotoxic assay	48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50=0.97 μM
MDA435/LCC6 cells	Proliferation assay		Antiproliferative activity against multidrug resistant MDA435/LCC6 cells by ELISA, IC50=1.442 μM
U937 cells	Cytotoxic assay		Cytotoxicity against human U937 cells by MTT assay, IC50=6.2 μM
A549 cells	Cytotoxic assay		Cytotoxicity against human A549 cells by MTT assay, IC50=7.8 μM
HT-29 cell line	Proliferation assay		Inhibitory concentration of compound against proliferation of colon carcinoma HT-29 cell line, IC50=8 μM
HepG2 cells	Proliferation assay	48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay, IC50=11.05 μM
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	444.48	화학식	C₂₂H₂₈N₄O₆	보관 (수령일로부터)	3년-20°C분말
CAS 번호	65271-80-9	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관

용해도

In vitro
배치:

DMSO : 88 mg/mL (197.98 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 89 mg/mL (200.23 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 22 mg/mL (49.49 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 88 mg/mL (197.98 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.100mg/ml (2.47mM)	Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

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

Targets/IC₅₀/Ki	Topo II (Cell-free assay)
시험관 내(In vitro)	Mitoxantrone은 연구된 모든 환자에서 DNA 단편화 및 캐스파제 활성화의 마커인 폴리(ADP-리보스) 폴리머라제(PARP)의 단백질 분해성 절단을 유도하여, Mitoxantrone의 세포독성 효과가 아폽토시스 유도에 의한 것임을 입증합니다. 이 화합물은 전골수성 백혈병 세포주 HL60에서 NFkappaB를 활성화하고 IkappaBalpha 분해를 촉진하지만, Topoisomerase II의 베타 이소폼이 없고 변형된 세포하 분포를 초래하는 잘린 알파 이소폼을 발현하는 변이 세포인 HL60/MX2 세포에서는 그렇지 않습니다. 이는 활성화된 PBMC, B 림프구 또는 항원 제시 세포(APC)에서 자극된 항원 특이적 T-세포주(TCL)의 증식을 용량 의존적으로 억제합니다. 이 화학 물질은 낮은 농도에서 PBMC, 단핵구 및 DC의 아폽토시스를 유도하는 반면, 고농도에서는 세포 용해를 유발합니다.
생체 내(In vivo)	Mitoxantrone은 마우스의 HID 이종이식편 성장률을 일시적으로 감소시키지만 PAC120 이종이식편에는 영향을 미치지 않습니다. 이 화합물은 자발적 고혈압 쥐에서 심장 병변, 신장병증 및 장 독성의 심각도를 유발합니다. 이 화학 물질과 철(III)은 강한 2:1 복합체를 형성하며, 이때 삼중 배위 리간드로 작용할 수 있습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/9450803/ [2] https://pubmed.ncbi.nlm.nih.gov/10940316/ [3] https://pubmed.ncbi.nlm.nih.gov/16171875/ [4] https://pubmed.ncbi.nlm.nih.gov/12686819/ [5] https://pubmed.ncbi.nlm.nih.gov/9299365/

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