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SN-38 Topoisomerase-I-Inhibitor

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

Kat.-Nr.S4908

SN-38 (NK012) ist ein aktiver Metabolit von CPT-11, hemmt die DNA-Topoisomerase I, die DNA-Synthese und verursacht häufig Einzelstrangbrüche der DNA. SN-38 induziert Autophagie.

SN-38 ADC Cytotoxin Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 392.4

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.96%

99.96

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

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	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
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	392.4	Formel	C₂₂H₂₀N₂O₅	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	86639-52-3	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	NK012			Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)O

Löslichkeit

In vitro
Charge:

DMSO : 19 mg/mL (48.41 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (127.42 mM) Mit 50°C Wasserbad erwärmt; Ultraschallbehandelt;
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 40 mg/mL (101.93 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 20 mg/mL (50.96 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 50 mg/mL (127.42 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus

Targets/IC₅₀/Ki	Topo I (Cell-free assay)
In vitro	SN-38, ein biologisch aktiver Metabolit von CPT-11. Diese Verbindung verursacht die stärkste Hemmung der DNA topoisomerase I, gefolgt von CPT und dann CPT-11. CPT-11 verschiebt die Position der entspannten DNA dosisabhängig in Richtung der geschnittenen DNA, aber diese Verbindung und CPT zeigen keinen Effekt auf die Position der entspannten DNA. Sie hemmt die DNA-Synthese dosis- und zeitabhängig. Die jeweiligen IC50-Werte dieser Chemikalie in der DNA-Synthese betragen 0,077 µM. Die hemmende Wirkung auf die RNA-Synthese ist geringer als die auf die DNA-Synthese und sie hemmt die Proteinsynthese nicht. Dieser Metabolit verursachte häufig Einzelstrangbrüche der DNA in P388-Zellen.
Kinase-Assay	Topoisomerase-I-Assay
Kinase-Assay	Eine Einheit (die Mindestmenge für die vollständige Entspannung von 0,5 μg SV40-DNA unter den Bedingungen dieser Studie) Topoisomerase I, 0,5 μL der Testsubstanzen und 0,5 μg SV40-DNA werden nacheinander zu dem Reaktionspuffer gegeben, der aus 25 mM Tris-HCl (pH 7,5), 50 mM KCl, 5 mM MgCl₂, 0,25 mM EDTA-Dinatriumsalz, 0,25 mM Dithiothreitol, 15 μg/mL Rinderserumalbumin und 5 % Glycerin besteht. Anschließend wird die Reaktionsmischung (50 μL) 10 min bei 37 °C inkubiert, und die Reaktion wird durch Behandlung mit 7,5 μL einer Lösung, bestehend aus 1 % Natriumdodecylsulfat, 20 mM EDTA-Dinatriumsalz und 0,5 mg/mL Proteinase K, für weitere 30 min bei 37 °C beendet. Die Proben werden mit 5 μL des Ladepuffers, der 10 mM Na₂HPO₄, 31,3 % Saccharose und 0,3 % Bromphenolblau enthält, gemischt. Entspannte (Form Ir) DNA wird von supercoiled (Form I) und geschnittener (Form II) DNA durch Elektrophorese auf 0,8 % Agarosegel bei 50 mA und 20 V für 17 h in Gegenwart von 2 μg/mL CHQ, 10 mM EDTA, 30 mM NaH₂PO₄ und 36 mM Tris-HCl (pH 7,8) getrennt. Nach der Elektrophorese wird das Gel mit 0,05 % Ethidiumbromid gefärbt und mit UV-Licht (302 nm) fotografiert. Die Menge an DNA wird mittels Densitometer quantifiziert.
In vivo	Nach oraler Verabreichung treten Spitzenkonzentrationen dieser Verbindung innerhalb von 1 Stunde auf, und der prozentuale Anteil des ungebundenen Lactons im murinen Plasma bei 1000 ng/mL beträgt 3,4 +/- 0,67 %, während bei 100 ng/mL der prozentuale Anteil des ungebundenen Lactons 1,18 +/- 0,14 % beträgt. Die Laktone-AUCs bei Mäusen mit humanen Neuroblastom-Xenotransplantaten sind größer als bei Tieren ohne Tumor.
Literatur	[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/

Anwendungen

Methoden	Biomarker	Bilder	PMID
Western blot	p-Chk1 / Chk1 / Topo I		18509065
Growth inhibition assay	Cell viability		25759163

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
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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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):