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Irinotecan Hydrochloride Trihydrate Topoisomerase I Inhibitor

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

N. Cat.S2217

Irinotecan HCl Trihydrate è un triidrato di cloridrato di irinotecan (Camptosar, Campto, CPT-11) che è un inibitore della Topoisomerase I con IC50 di 15,8 e 5,17 μM rispettivamente per le cellule LoVo e le cellule HT-29.

Irinotecan Hydrochloride Trihydrate Topoisomerase inibitore Chemical Structure

Struttura chimica

Peso molecolare: 677.18

Vai a

Controllo Qualità

Lotto: Purezza: 99.97%

99.97

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

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	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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Informazioni chimiche, conservazione e stabilità

Peso molecolare	677.18	Formula	C₃₃H₃₈N₄O₆.HCl.3H₂O	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	136572-09-3	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità

In vitro
Lotto:

DMSO : 100 mg/mL (147.67 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 187.5 mg/mL (276.88 mM) Riscaldato con bagno dacqua a 50°C; Sonicato;
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 5 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Caratteristiche	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I
In vitro	Irinotecan viene attivato a SN-38 dalle carbossilesterasi per poter interagire con il suo bersaglio, la Topoisomerase I. Irinotecan induce quantità simili di complessi clivabili al suo IC50 nelle cellule LoVo e nelle linee cellulari HT-29. SN-38 induce una formazione concentrazione-dipendente di complessi clivabili, che non è significativamente diversa nelle cellule LoVo e nelle linee cellulari HT-29. L'accumulo cellulare di Irinotecan è marcatamente diverso, raggiungendo livelli costantemente più elevati nelle cellule HT-29 rispetto alle cellule LoVo. L'anello E lattonico di Irinotecan e SN-38 si idrolizza reversibilmente in soluzioni acquose, e l'interconversione tra le forme lattonica e carbossilica dipende dal pH e dalla temperatura. Il fegato è il principale responsabile dell'attivazione di Irinotecan a SN-38. A parità di concentrazioni di Irinotecan e SN-38 glucuronide, la velocità di produzione di SN-38 mediata dalla beta-glucuronidasi è maggiore di quella formata da Irinotecan sia nel tessuto tumorale che normale. Irinotecan viene convertito a SN-38 anche nell'intestino, nel plasma e nei tessuti tumorali. Irinotecan è significativamente più attivo nelle cellule SCLC che nelle linee cellulari NSCLC, mentre non si osserva alcuna differenza significativa tra i tipi istologici con SN-38.
In vivo	Negli xenotrapianti COLO 320, Irinotecan induce un'inibizione massima della crescita del 92%. Una singola dose di Irinotecan aumenta significativamente le quantità di Topoisomerase I legata covalentemente al DNA nello stomaco, nel duodeno, nel colon e nel fegato. Contestualmente, il gruppo trattato con Irinotecan mostra quantità significativamente maggiori di rotture del filamento di DNA nelle cellule della mucosa del colon rispetto al gruppo di controllo.
Riferimenti	[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/

Applicazioni

Metodi	Biomarcatori	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

Informazioni sullo studio clinico

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

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