연구용

SN-38 Topoisomerase I 억제제

Name: SN-38
Brand: Selleck Chemicals
SKU: S4908
Rating: 5 (100 reviews)

제품 번호S4908

SN-38 (NK012)은 CPT-11의 활성 대사물질로, DNA topoisomerase I, DNA 합성을 억제하고 빈번한 DNA 단일 가닥 절단을 유발합니다. SN-38은 autophagy를 유도합니다.

SN-38 ADC Cytotoxin 억제제 Chemical Structure

화학 구조

분자량: 392.4

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품질 관리

배치: 순도: 99.96%

99.96

관련 타겟	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis Topoisomerase PPAR Sirtuin Casein Kinase
기타 ADC Cytotoxin 억제제	Triptolide Luteolin (+)-Bicuculline Rutin Artemisinin BHQ Pinocembrin Harmine hydrochloride Luteoloside Sacituzumab-govitecan

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
human DU145 prostate cell line	Proliferation assay			Antiproliferative activity against human DU145 prostate cell line, IC50=13 nM	10498216
human MCF-7 breast cell line	Proliferation assay			Antiproliferative activity against human MCF-7 breast cell line, IC50=0.37 μM	10498216
human SKOV-3 ovarian cell line	Proliferation assay			Antiproliferative activity against human SKOV-3 ovarian cell line, IC50=0.72 μM	10498216
human breast cancer cell line (SK-BR-3)	Cytotoxic assay			In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3), IC50=4 nM	11334569
human lung cancer cell line (H128)	Cytotoxic assay			In Vitro cytotoxicity against human lung cancer cell line (H128), IC50=6 nM	11334569
human stomach cancer cell line (MKN45)	Cytotoxic assay			In Vitro cytotoxicity against human stomach cancer cell line (MKN45), IC50=8 nM	11334569
human ovarian cancer cell line (SK-OV-3)	Cytotoxic assay			In Vitro cytotoxicity against human ovarian cancer cell line (SK-OV-3), IC50=11 nM	11334569
human colon cancer cell line (WiDr)	Cytotoxic assay			In Vitro cytotoxicity against human colon cancer cell line (WiDr), IC50=14 nM	11334569
human lung cancer cell line (A549)	Cytotoxic assay			In Vitro cytotoxicity against human lung cancer cell line (A549)	11334569
NSCLC-H460	Cytotoxic assay			Cytotoxicity against human non-small-cell lung carcinoma cell line H460 (NSCLC-H460), IC50=80 nM	11563925
PC-3 carcinoma cell line	Growth inhibition assay			Concentration required to inhibit growth of human prostate PC-3 carcinoma cell line, IC50=35.6 nM	15454230
human HCT116 colon cancer cell line	Function assay			Inhibitory concentration against human HCT116 colon cancer cell line, IC50=7 nM	15808456
human Bel-7402 liver cancer cell line	Function assay			Inhibitory concentration against human Bel-7402 liver cancer cell line, IC50=3.19 μM	15808456
human tumor HL60 cell-line	Function assay		3 days	In-vitro inhibitory concentration for human tumor HL60 cell-line was determined using SRB assay after 3 days of incubation, IC50=19 nM	15913996
human H460 cell	Growth inhibition assay			Inhibition of human H460 cell growth, IC50=80 nM	16913706
MDA-MB-435	Function assay			Inhibition against MDA-MB-435 S human breast cancer cells in the absence of albumin, IC50 = 0.005 μM.	11052802
MDA-MB-435	Function assay			Inhibition against MDA-MB-435 S human breast cancer cells in the presence of 30 mg/mL HSA, IC50 = 0.05 μM.	11052802
PC-6/SN2-5H	Function assay			TP_TRANSPORTER: uptake in membrane vesicle from PC-6/SN2-5H cells, Km = 4 μM.	11688982
HT-29	Function assay			In vitro inhibitory concentration required against HT-29 human colon cancer cells, IC50 = 0.0273 μM.	12617927
SaoS2	Function assay			TP_TRANSPORTER: drug resistance(Imatinib mesylate) in BCRP-expressing SaoS2 cells, IC50 = 0.176 μM.	15059881
DU145	Antiproliferative assay		96 hrs	Antiproliferative activity against human DU145 cells after 96 hrs, IC50 = 0.004 μM.	18276141
MIA PaCa	Antiproliferative assay		96 hrs	Antiproliferative activity against human MIA PaCa cells after 96 hrs, IC50 = 0.006 μM.	18276141
HT29	Antiproliferative assay		96 hrs	Antiproliferative activity against human HT29 cells after 96 hrs, IC50 = 0.012 μM.	18276141
H460	Antiproliferative assay		1 hr	Antiproliferative activity against human H460 cells after 1 hr of drug exposure measured after 72 hrs, IC50 = 0.22 μM.	18424133
HT29	Antiproliferative assay		1 hr	Antiproliferative activity against human HT29 cells after 1 hr of drug exposure measured after 72 hrs, IC50 = 0.67 μM.	18424133
HT29	Antiproliferative assay		1 hr	Antiproliferative activity against BCRP overexpressing mitoxantrone-resistant human HT29 cells after 1 hr of drug exposure measured after 72 hrs, IC50 = 11.5 μM.	18424133
H460	Cytotoxicity assay			Cytotoxicity against human H460 cells, IC50 = 0.22 μM.	18434153
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells by SRB method, IC50 = 0.08 μM.	18986807
HT-29	Cytotoxicity assay			Cytotoxicity against human HT-29 cells by SRB method, IC50 = 0.12 μM.	18986807
PC6	Antiproliferative assay		6 days	Antiproliferative activity against human PC6 cells carrying pRC after 6 days, IC50 = 0.00043 μM.	19254843
HCT116	Antiproliferative assay		3 days	Antiproliferative activity against human HCT116 cells after 3 days, IC50 = 0.00055 μM.	19254843
QG56	Antiproliferative assay		3 days	Antiproliferative activity against human QG56 cells after 3 days, IC50 = 0.0028 μM.	19254843
NCI-H460	Antiproliferative assay		3 days	Antiproliferative activity against human NCI-H460 cells after 3 days, IC50 = 0.0033 μM.	19254843
BCRP	Antiproliferative assay		6 days	Antiproliferative activity against human PC6 expressing BCRP cells after 6 days, IC50 = 0.0051 μM.	19254843
KB3-1	Cytotoxicity assay		4 days	Cytotoxicity against human KB3-1 cells after 4 days by MTT method, IC50 = 0.004 μM.	19303306
KBV1	Cytotoxicity assay		4 days	Cytotoxicity against MDR1 overexpressing human KBV1 cells after 4 days by MTT method, IC50 = 0.046 μM.	19303306
KBH5.0	Cytotoxicity assay		4 days	Cytotoxicity against BCRP overexpressing human KBH5.0 cells after 4 days by MTT method, IC50 = 0.3 μM.	19303306
NCI-H460	Antiproliferative assay		1 hr	Antiproliferative activity against human NCI-H460 cells after short term exposure for 1 hr measured after 72 hrs in drug-free medium, IC50 = 0.13 μM.	19530720
A549/ATCC	Antitumor assay			Antitumor activity against human A549/ATCC cells by SRB method, IC50 = 0.088 μM.	19541483
HT-29	Antitumor assay			Antitumor activity against human HT-29 cells by SRB method, IC50 = 0.17 μM.	19541483
gastric cancer cells	Growth inhibition assay		72 hrs	Growth inhibition of human gastric cancer cells after 72 hrs by sulforhodamine B assay, GI50 = 0.066 μM.	20884089
lung cancer cells	Growth inhibition assay		72 hrs	Growth inhibition of human lung cancer cells after 72 hrs by sulforhodamine B assay, GI50 = 0.066 μM.	20884089
colon cancer cells	Growth inhibition assay		72 hrs	Growth inhibition of human colon cancer cells after 72 hrs by sulforhodamine B assay, GI50 = 0.066 μM.	20884089
HT-29	Cytotoxicity assay			Cytotoxicity against human HT-29 cells, IC50 = 0.0059 μM.	21470864
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells, IC50 = 0.047 μM.	21470864
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells expressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50 = 0.0026 μM.	22959246
A2780	Cytotoxicity assay		72 hrs	Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50 = 0.009 μM.	22959246
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells, IC50 = 0.03 μM.	23578545
HT-29	Cytotoxicity assay			Cytotoxicity against human HT-29 cells, IC50 = 0.03 μM.	23578545
L1210	Cytotoxicity assay			Cytotoxicity against mouse L1210 cells, IC50 = 0.04 μM.	23578545
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells assessed as inhibition of cell viability after 72 hrs by MTS assay, IC50 = 0.11 μM.	23622981
DU145	Function assay	0.1 to 0.5 uM	24 hrs	Inhibition of HDAC in human DU145 cells assessed as upregulation of p21waf1 expression at 0.1 to 0.5 uM after 24 hrs by Western blot analysis	23622981
A549	Cytotoxicity assay		3 days	Cytotoxicity against human A549 cells assessed as growth inhibition after 3 days by SRB assay, IC50 = 0.00272 μM.	24529870
HCT116	Cytotoxicity assay		3 days	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 3 days by SRB assay, IC50 = 0.031 μM.	24529870
HT-29	Cytotoxicity assay		3 days	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 3 days by SRB assay, IC50 = 0.10667 μM.	24529870
HCT116	Cytotoxicity assay			Cytotoxicity against human HCT116 cells, IC50 = 0.166 μM.	24529870
MDA-MB-231	Cytotoxicity assay			Cytotoxicity against human MDA-MB-231 cells, IC50 = 0.176 μM.	24529870
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells, IC50 = 0.259 μM.	24529870
HEK293	Cytotoxicity assay		72 hrs	Intrinsic cytotoxicity against HEK293 cells assessed as reduction in cell viability after 72 hrs by MTT assay, IG50 = 0.005 μM.	25272055
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.00428 μM.	25835359
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.01854 μM.	25835359
HCT15	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT15 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.008 μM.	27060760
U251	Cytotoxicity assay		72 hrs	Cytotoxicity against human U251 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.021 μM.	27060760
U87MG	Cytotoxicity assay		72 hrs	Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.03 μM.	27060760
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.054 μM.	27060760
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 0.515 μM.	27060760
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50 = 1.97 μM.	27060760
NCI-H460	Cytotoxicity assay		24 hrs	Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50 = 0.05 μM.	28350997
NCI-H460	Cytotoxicity assay		24 hrs	Cytotoxicity against human NCI-H460 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50 = 0.06 μM.	28350997
HT-29	Cytotoxicity assay		24 hrs	Cytotoxicity against human HT-29 cells pretreated for 24 hrs under normoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50 = 2.74 μM.	28350997
HT-29	Cytotoxicity assay		24 hrs	Cytotoxicity against human HT-29 cells pretreated for 24 hrs under hypoxic condition followed by compound washout measured after 72 hrs by MTT assay, IC50 = 3.71 μM.	28350997
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H460 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay, IC50 = 0.047 μM.	28740613
NCI-H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human NCI-H460 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay, IC50 = 0.05 μM.	28740613
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as growth reduction under normoxic condition after 72 hrs by MTT assay, IC50 = 0.096 μM.	28740613
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells assessed as growth reduction under hypoxic condition after 72 hrs by MTT assay, IC50 = 0.119 μM.	28740613
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells	29435139
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 0.00078 μM.	30115492
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50 = 0.00162 μM.	30115492
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.0001 μM.	30169038
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, IC50 = 0.2 μM.	30169038
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	392.4	화학식	C₂₂H₂₀N₂O₅	보관 (수령일로부터)	3년-20°C분말
CAS 번호	86639-52-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	NK012			Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)O

용해도

In vitro
배치:

DMSO : 19 mg/mL (48.41 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (127.42 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 40 mg/mL (101.93 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (50.96 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (127.42 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.
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.	0.630mg/ml (1.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 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 make it clear. Volume up 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 I (Cell-free assay)
시험관 내(In vitro)	SN-38은 CPT-11의 생물학적 활성 대사 물질입니다. 이 화합물은 DNA topoisomerase I의 가장 강력한 억제를 유발하며, CPT, 그리고 CPT-11 순으로 나타납니다. CPT-11은 이완된 DNA의 위치를 용량 의존적으로 잘린 DNA 방향으로 이동시키지만, 이 화합물과 CPT는 이완된 DNA의 위치에 영향을 미치지 않습니다. 이는 DNA 합성을 용량 의존적 및 시간 의존적으로 억제합니다. 이 화학 물질의 DNA 합성에서 각각의 IC50 값은 0.077 µM입니다. RNA 합성에 대한 억제 효과는 DNA 합성보다 적으며 단백질 합성은 억제하지 않습니다. 이 대사 물질은 P388 세포에서 빈번한 DNA 단일 가닥 절단을 유발했습니다.
키나아제 분석	Topoisomerase I 분석
키나아제 분석	Topoisomerase I 1단위 (이 연구 조건 하에서 0.5 μg SV40 DNA의 완전한 이완을 위한 최소량), 시험 화합물 0.5 μL, SV40 DNA 0.5 μg을 반응 완충액에 순차적으로 첨가합니다. 반응 완충액은 25 mM Tris-HCl (pH 7.5), 50 mM KC1, 5 mM MgCl₂, 0.25 mM EDTA 이나트륨 염, 0.25 mM DTT (dithiothreitol), 15 μg/mL 소 혈청 알부민, 5% 글리세롤로 구성됩니다. 그 후, 반응 혼합물 (50 μL)을 37 °C에서 10분 동안 배양하고, 반응은 1% SDS (sodium dodecyl sulfate), 20 mM EDTA 이나트륨 염, 0.5 mg/mL 프로테이나제 K로 구성된 용액 7.5 μL로 37 °C에서 추가로 30분 동안 처리하여 종료합니다. 샘플은 10 mM Na₂HPO₄, 31.3% sucrose, 0.3% bromophenol blue를 포함하는 로딩 버퍼 5 μL와 혼합됩니다. 이완된 (form Ir) DNA는 0.8% 아가로스 젤에서 50 mA, 20 V로 17시간 동안 2 μg/mL CHQ, 10 mM EDTA, 30 mM NaH₂PO₄, 36 mM Tris-HCl (pH 7.8) 존재 하에 전기영동하여 초나선형 (form I) 및 잘린 (form II) DNA와 분리됩니다. 전기영동 후, 젤은 0.05% 에티듐 브로마이드로 염색하고 UV 라이트 (302 nm)로 촬영합니다. DNA 양은 덴시토미터를 사용하여 정량화됩니다.
생체 내(In vivo)	경구 투여 후, 이 화합물의 최고 농도는 1시간 이내에 발생하며, 1000 ng/mL에서 생쥐 혈장 내 비결합 락톤의 백분율은 3.4 +/- 0.67%인 반면, 100 ng/mL에서는 비결합 백분율이 1.18 +/- 0.14%입니다. 인간 신경모세포종 이종이식을 지닌 생쥐의 락톤 AUC는 종양을 지니지 않은 동물보다 더 높습니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/1651156/ [2] http://www.ncbi.nlm.nih.gov/pubmed/ 9219511 [3] https://pubmed.ncbi.nlm.nih.gov/12712458/ [4] https://pubmed.ncbi.nlm.nih.gov/30587986/

적용 분야

방법	바이오마커	이미지	PMID
Western blot	p-Chk1 / Chk1 / Topo I		18509065
Growth inhibition assay	Cell viability		25759163

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT06143774	Recruiting	Advanced Solid Tumor	TaiRx Inc.	October 31 2023	Phase 1
NCT05101096	Recruiting	Advanced Solid Tumor\|Metastatic Triple-Negative Breast Cancer\|HR+/HER2- Metastatic Breast Cancer\|Metastatic Urothelial Cancer	Gilead Sciences	October 20 2021	Phase 1\|Phase 2
NCT05119907	Recruiting	Solid Tumor	Gilead Sciences	October 12 2021	Phase 2
NCT04866641	Recruiting	Advanced Solid Tumor	Taivex Therapeutics Corporation	June 24 2021	Phase 1
NCT04617522	Recruiting	Advanced or Metastatic Solid Tumor\|Liver Failure	Gilead Sciences	April 6 2021	Phase 1

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