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Irinotecan Hydrochloride Trihydrate Topoisomerase I Inhibitor

Name: Irinotecan Hydrochloride Trihydrate
Brand: Selleck Chemicals
SKU: S2217
Rating: 5 (90 reviews)

Réf. CatalogueS2217

Irinotecan HCl Trihydrate est un chlorhydrate trihydraté d'Irinotecan (Camptosar, Campto, CPT-11) qui est un inhibiteur de la Topoisomerase I avec une IC50 de 15,8 et 5,17 μM pour les cellules LoVo et les cellules HT-29, respectivement.

Irinotecan Hydrochloride Trihydrate Topoisomerase inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 677.18

Aller à

Contrôle Qualité

Lot : Pureté : 99.97%

99.97

Cibles apparentées	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Autre Topoisomerase Inhibiteurs	Camptothecin (CPT) Betulinic acid Beta-Lapachone (S)-10-Hydroxycamptothecin Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Cu(II)-Elesclomol Hydroxy Camptothecine Rubitecan

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Description de lactivité	PMID
RPMI8402	Cytotoxicity assay		4 days	Cytotoxic activity against human lymphoblast tumor cell line RPMI8402 after 4 days of treatment. IC50=0.57 μM	12747798
Hep3B	Antiproliferative assay		72 hrs	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM.	19796956
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM.	19796956
NCI60	Growth inhibition assay			Growth inhibition of human NCI60 cells by SBR assay, GI50 = 14.1254 μM.	21035334
Hep3B	Growth inhibition assay		72 hrs	Growth inhibition of human Hep3B cells after 72 hrs by XTT assay, GI50 = 4.73 μM.	22079254
HepG2	Growth inhibition assay		72 hrs	Growth inhibition of human HepG2 cells after 72 hrs by XTT assay, GI50 = 5.94 μM.	22079254
MDA-MB-231	Growth inhibition assay		72 hrs	Growth inhibition of human MDA-MB-231 cells after 72 hrs by XTT assay, GI50 = 9.17 μM.	22079254
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells incubated for 72 hrs by MTT assay, GI50 = 5 μM.	22867019
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells incubated for 72 hrs by MTT assay, GI50 = 7.1 μM.	22867019
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50 = 12.2 μM.	22867019
K562	Antiproliferative assay		72 hrs	Antiproliferative activity against human K562 cells after 72 hrs, GI50 = 1.9 μM.	25420175
A549	Antitumor assay		4 hrs	Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50 = 6.528 μM.	18207748
LOVO	Antitumor assay		4 hrs	Antitumor activity against human LOVO cells after 4 hrs by MTT assay, IC50 = 9.015 μM.	18207748
MCF7	Antitumor assay		4 hrs	Antitumor activity against human MCF7 cells after 4 hrs by MTT assay, IC50 = 17.403 μM.	18207748
LS174T	Cytotoxicity assay		96 hrs	Cytotoxicity against human LS174T cells after 96 hrs by MTT assay, IC50 = 1.16 μM.	18513976
KB3-1	Cytotoxicity assay			Cytotoxicity against human KB3-1 cells by MTT method, IC50 = 0.68 μM.	18771930
KBH5.0	Cytotoxicity assay			Cytotoxicity against human KBH5.0 cells by MTT method, IC50 = 7.4 μM.	18771930
KBV1	Cytotoxicity assay			Cytotoxicity against human KBV1 cells by MTT method, IC50 = 40 μM.	18771930
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 1.14 μM.	20371183
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 4.61 μM.	20371183
LoVo	Cytotoxicity assay		72 hrs	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50 = 4.99 μM.	20371183
A549	Cytotoxicity assay		3 days	Cytotoxicity against human A549 cells after 3 days by MTT assay, IC50 = 6.4 μM.	20942490
LoVo	Cytotoxicity assay		3 days	Cytotoxicity against human LoVo cells after 3 days by MTT assay, IC50 = 8.8 μM.	20942490
MDA-MB-435	Cytotoxicity assay		3 days	Cytotoxicity against human MDA-MB-435 cells after 3 days by MTT assay, IC50 = 17 μM.	20942490
A375	Cytotoxicity assay		72 hrs	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM.	21341674
PC3	Cytotoxicity assay		72 hrs	Cytotoxicity against human PC3 cells after 72 hrs by alamar blue assay, IC50 = 0.004 μM.	21341674
LNCAP	Cytotoxicity assay		72 hrs	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50 = 0.009 μM.	21341674
MESSA	Cytotoxicity assay		72 hrs	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50 = 0.01 μM.	21341674
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay, IC50 = 0.015 μM.	21341674
H69	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50 = 0.022 μM.	21341674
MES-SA/Dx5	Cytotoxicity assay		72 hrs	Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.022 μM.	21341674
H460	Cytotoxicity assay		72 hrs	Cytotoxicity against human H460 cells after 72 hrs by alamar blue assay in presence of 40 mg/ml HSA, IC50 = 0.027 μM.	21341674
IGROV1	Cytotoxicity assay		72 hrs	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50 = 0.03 μM.	21341674
SK-MEL-2	Cytotoxicity assay		72 hrs	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50 = 0.1 μM.	21341674
MALME-3M	Cytotoxicity assay		72 hrs	Cytotoxicity against human MALME-3M cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM.	21341674
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by alamar blue assay, IC50 = 0.2 μM.	21341674
HT-29	Cytotoxicity assay		72 hrs	Cytotoxicity against human HT-29 cells after 72 hrs by alamar blue assay, IC50 = 0.22 μM.	21341674
H69AR	Cytotoxicity assay		72 hrs	Cytotoxicity against human H69AR cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50 = 0.25 μM.	21341674
DU145	Cytotoxicity assay			Cytotoxicity against human DU145 cells by SRB assay, IC50 = 9.3 μM.	23102893
A549	Cytotoxicity assay			Cytotoxicity against human A549 cells by SRB assay, IC50 = 9.48 μM.	23102893
KB	Cytotoxicity assay			Cytotoxicity against human KB cells by SRB assay, IC50 = 9.83 μM.	23102893
HEK293	Inhibition of human		1.5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in HEK293 cells after 1.5 mins by scintillation counting analysis, IC50 = 2.1 μM.	23241029
HEK293	Inhibition of human		3 mins	Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 2.7 μM.	23241029
MDCK2	Inhibition of human		5 mins	Inhibition of human MATE1-mediated [14]-metformin uptake expressed in polarized MDCK2 cells after 5 mins by liquid scintillation counting analysis, IC50 = 4.3 μM.	23241029
HEK293	Inhibition of human	up to 500 uM	1.5 mins	Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells up to 500 uM after 1.5 mins by fluorescence assay, IC50 = 7.9 μM.	23241029
HEK293	Inhibition of human		1.5 mins	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50 = 7.9 μM.	23241029
HEK293	Inhibition of human		3 mins	Inhibition of human OCT1-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay, IC50 = 20.8 μM.	23241029
H3347	Cytotoxicity assay		72 hrs	Cytotoxicity against human H3347 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 7.53 μM.	24583355
DLD1	Cytotoxicity assay		72 hrs	Cytotoxicity against human DLD1 cells assessed as growth inhibition after 72 hrs by Alamar Blue assay, IC50 = 25.1 μM.	24583355
DU145	Cytotoxicity assay		72 hrs	Cytotoxicity against human DU145 cells after 72 hrs by SRB assay, IC50 = 9.3 μM.	25003995
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 9.5 μM.	25003995
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 9.8 μM.	25003995
MDA-MB-435	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, IC50 = 6.3 μM.	26226379
HCT116	Cytotoxicity assay		72 hrs	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 18.6 μM.	26226379
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by MTT assay, IC50 = 20.1 μM.	26226379
HCT116	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human HCT116 cells after 24 to 72 hrs by SRB assay, IC50 = 2 μM.	26595875
RKO	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human RKO cells after 24 to 72 hrs by SRB assay, IC50 = 6.2 μM.	26595875
HCT15	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human HCT15 cells after 24 to 72 hrs by SRB assay, IC50 = 8.5 μM.	26595875
SW480	Antiproliferative assay		24 to 72 hrs	Antiproliferative activity against human SW480 cells after 24 to 72 hrs by SRB assay, IC50 = 12.3 μM.	26595875
PC3	Antiproliferative assay		72 hrs	Antiproliferative activity against human PC3 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 0.8 μM.	26731300
MCF7	Antiproliferative assay		96 hrs	Antiproliferative activity against human MCF7 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 0.9 μM.	26731300
T84	Antiproliferative assay		96 hrs	Antiproliferative activity against human T84 cells assessed as cellular DNA content after 96 hrs by CyQUANT NF fluorescence assay, IC50 = 1.2 μM.	26731300
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells assessed as cellular DNA content after 72 hrs by CyQUANT NF fluorescence assay, IC50 = 1.9 μM.	26731300
MCF7	Cytotoxicity assay		24 hrs	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.5 μM.	26841168
A549	Cytotoxicity assay		24 hrs	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.8 μM.	26841168
HepG2	Cytotoxicity assay		24 hrs	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 0.9 μM.	26841168
SW480	Cytotoxicity assay		24 hrs	Cytotoxicity against human SW480 cells assessed as reduction in cell viability after 24 hrs by MTS assay, IC50 = 1.4 μM.	26841168
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.48 μM.	26994847
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B colorimetric assay, IC50 = 9.828 μM.	26994847
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by sulforhodamine B assay, IC50 = 7.99 μM.	28285912
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B assay, IC50 = 8.3 μM.	28285912
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by sulforhodamine B assay, IC50 = 11.3 μM.	28285912
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B assay, IC50 = 15.6 μM.	28285912
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 6.3 μM.	28351590
ZR-7530	Antiproliferative assay		72 hrs	Antiproliferative activity against human ZR-7530 cells after 72 hrs by MTT assay, IC50 = 18 μM.	28351590
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50 = 20 μM.	28351590
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM.	28789891
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.31 μM.	28789891
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.32 μM.	28789891
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.56 μM.	28789891
KB	Cytotoxicity assay		72 hrs	Cytotoxicity against human KB cells after 72 hrs by SRB assay, IC50 = 7.99 μM.	28927790
A549	Cytotoxicity assay		72 hrs	Cytotoxicity against human A549 cells after 72 hrs by SRB assay, IC50 = 8.3 μM.	28927790
MCF7	Cytotoxicity assay		72 hrs	Cytotoxicity against human MCF7 cells after 72 hrs by SRB assay, IC50 = 11.3 μM.	28927790
MDA-MB-231	Cytotoxicity assay		72 hrs	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by SRB assay, IC50 = 15.6 μM.	28927790
Maver2	Antiproliferative assay		72 hrs	Antiproliferative activity against human Maver2 cells after 72 hrs by MTT assay, IC50 = 0.74 μM.	29150335
NB4	Antiproliferative assay		72 hrs	Antiproliferative activity against human NB4 cells after 72 hrs by MTT assay, IC50 = 1 μM.	29150335
Capan1	Antiproliferative assay		72 hrs	Antiproliferative activity against human Capan1 cells after 72 hrs by SRB assay, IC50 = 1.5 μM.	29150335
NCI-H460	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H460 cells after 72 hrs by SRB assay, IC50 = 2.4 μM.	29150335
DU145	Antiproliferative assay		72 hrs	Antiproliferative activity against human DU145 cells after 72 hrs by SRB assay, IC50 = 2.8 μM.	29150335
A2780	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780 cells after 72 hrs by SRB assay, IC50 = 3.8 μM.	29150335
HepG2	Antiproliferative assay		72 hrs	Antiproliferative activity against human HepG2 cells after 72 hrs by SRB assay, IC50 = 4 μM.	29150335
A431	Antiproliferative assay		72 hrs	Antiproliferative activity against human A431 cells after 72 hrs by SRB assay, IC50 = 4.1 μM.	29150335
U2932	Antiproliferative assay		72 hrs	Antiproliferative activity against human U2932 cells after 72 hrs by MTT assay, IC50 = 4.4 μM.	29150335
HT-29	Antiproliferative assay		72 hrs	Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50 = 4.8 μM.	29150335
HeLa	Antiproliferative assay		72 hrs	Antiproliferative activity against human HeLa cells after 72 hrs by SRB assay, IC50 = 5.8 μM.	29150335
MM487	Antiproliferative assay	10 uM	72 hrs	Antiproliferative activity against human MM487 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 9.4 μM.	29150335
MM432	Antiproliferative assay	10 uM	72 hrs	Antiproliferative activity against human MM432 cells at 10 uM after 72 hrs by MTT assay relative to control, IC50 = 10 μM.	29150335
A2780/DX	Antiproliferative assay		72 hrs	Antiproliferative activity against human A2780/DX cells after 72 hrs by SRB assay, IC50 = 20.1 μM.	29150335
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 1.63347 μM.	30115492
A549	Antiproliferative assay		72 hrs	Antiproliferative activity against human A549 cells after 72 hrs by SRB assay, IC50 = 1.88093 μM.	30115492
colon cancer cells	Cytotoxicity assay			Compound was tested in vitro for cytotoxicity against HCT116, human colon cancer cells (taxol-resistant) at a drug concentration producing 50% inhibition of colony formation, ID50 = 0.54 μM.	11965362
SW620	Antitumor assay	12.5 mg/kg		Antitumor activity against human SW620 cells xenografted in nude SCID mouse assessed as delay in tumor growth at 12.5 mg/kg, ip	22111927
HT-29	Antitumor assay	60 mg/kg	2 days	Antitumor activity against human HT-29 cells xenografted in nude mouse assessed as tumor growth inhibition at 60 mg/kg, iv tid administered 2 days measured on day 20	23360284
BT-483	Function assay	1 uM	24 hrs	Induction of DNA damage in human BT-483 cells assessed as gamma H2AX phosphorylation at Ser139 at 1 uM after 24 hrs by Western blot analysis	23419737
HCT116	Antitumor assay	30 mg/kg	6 days	Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days	24583355
H3347	Antitumor assay	30 mg/kg	6 days	Antitumor activity against human H3347 cells xenografted in nude mouse assessed as survival at 30 mg/kg,iv qd administered for 6 days	24583355
HCT116	Antitumor assay	100 mg/kg		Antitumor activity against human HCT116 cells xenografted in nu/nu mouse assessed as tumor regression at 100 mg/kg, iv dosed once every week	25003995
NCI-H526	Antitumor assay	30 mg/kg		Antitumor activity against human NCI-H526 cells xenografted in athymic nude mouse at 30 mg/kg, iv qd administered 5 times for every 2 days	28064078
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
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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SK-N-SH cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for MG 63 (6-TG R) 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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
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Informations chimiques, stockage et stabilité

Poids moléculaire	677.18	Formule	C₃₃H₃₈N₄O₆.HCl.3H₂O	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	136572-09-3	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	CPT-11 HCl Trihydrate			Smiles	CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7.O.O.O.Cl

Solubilité

In vitro
Lot:

DMSO : 100 mg/mL (147.67 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 187.5 mg/mL (276.88 mM) Réchauffé avec un bain-marie à 50°C; Ultrasonifié;
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 5 mg/mL

Water : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (7.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 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 make it clear; 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.
Clear solution	2%DMSO 1 98%Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	0.200mg/ml (0.30mM)	Taking the 1 mL working solution as an example, add 20 μL of 10 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. 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.
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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Caractéristiques	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I
In vitro	Irinotecan est activé en SN-38 par les carboxylesterases pour pouvoir interagir avec sa cible, la Topoisomerase I. Irinotecan induit des quantités similaires de complexes clivables à son IC50 dans les cellules LoVo et les lignées cellulaires HT-29. Le SN-38 induit une formation concentration-dépendante de complexes clivables, qui n'est pas significativement différente dans les cellules LoVo et les lignées cellulaires HT-29. L'accumulation cellulaire d'Irinotecan est nettement différente, atteignant des niveaux constamment plus élevés dans les cellules HT-29 que dans les cellules LoVo. L'anneau E lactone de l'Irinotecan et du SN-38 s'hydrolyse réversiblement dans les solutions aqueuses, et l'interconversion entre les formes lactone et carboxylate dépend du pH et de la température. Le foie est principalement responsable de l'activation de l'Irinotecan en SN-38. À concentrations égales d'Irinotecan et de glucuronide de SN-38, le taux de production de SN-38 médiée par la bêta-glucuronidase est plus élevé que celui formé à partir de l'Irinotecan, à la fois dans les tissus tumoraux et normaux. L'Irinotecan est également converti en SN-38 dans les intestins, le plasma et les tissus tumoraux. L'Irinotecan est significativement plus actif dans le cancer du poumon à petites cellules (SCLC) que dans les lignées cellulaires de cancer du poumon non à petites cellules (NSCLC), alors qu'aucune différence significative entre les types histologiques n'est observée avec le SN-38.
In vivo	Dans les xénogreffes COLO 320, l'Irinotecan induit une inhibition maximale de la croissance de 92%. Une dose unique d'Irinotecan augmente significativement les quantités de Topoisomerase I liée de manière covalente à l'ADN dans l'estomac, le duodénum, le côlon et le foie. Concomitamment, le groupe traité par Irinotecan montre des quantités significativement plus élevées de cassures de brins d'ADN dans les cellules de la muqueuse du côlon par rapport au groupe témoin.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/11914913/ [2] https://pubmed.ncbi.nlm.nih.gov/16842384/ [3] https://pubmed.ncbi.nlm.nih.gov/15182436/ [4] https://pubmed.ncbi.nlm.nih.gov/9649129/ [5] https://pubmed.ncbi.nlm.nih.gov/9033637/ [6] https://pubmed.ncbi.nlm.nih.gov/21046105/ [7] https://pubmed.ncbi.nlm.nih.gov/16317751/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	TopI / pAKT / pMEK / pERK / p-p38 MAPK / pJNK2 NFκB p65 / phospho-NFκB p65 / NFκB p50 / IκBα / p27Kip1 AMPK / p-AMPK / mTOR / p-mTOR / p70S6K / p-p70S6K	29237470
Immunofluorescence	NFκB	22206574
Growth inhibition assay	Cell viability	25973791

Informations sur lessai clinique

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT05854498	Recruiting	Metastatic Colorectal Cancer	University of Wisconsin Madison\|Ipsen	October 13 2023	Phase 2
NCT05732129	Not yet recruiting	Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer	Fudan University	March 1 2023	Phase 2
NCT05731518	Recruiting	Small Cell Lung Cancer	Biocity Biopharmaceutics Co. Ltd.	February 23 2023	Phase 1\|Phase 2
NCT06003998	Recruiting	Colorectal Cancer\|Peritoneal Metastases	Catharina Ziekenhuis Eindhoven	December 27 2022	Phase 2
NCT05277766	Recruiting	Peritoneal Carcinomatosis\|Peritoneal Metastases\|Colorectal Cancer\|Small Bowel Cancer\|Appendix Cancer\|Gastric Cancer\|Pancreatic Cancer\|Bile Duct Cancer	University Hospital Ghent\|Kom Op Tegen Kanker\|University Ghent	November 21 2022	Phase 1
NCT05379790	Recruiting	Gastric Cancer\|Peritoneal Metastases	Erasmus Medical Center	May 25 2022	Phase 1

Support technique

Instructions de manipulation

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