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Irinotecan Hydrochloride Trihydrate Topoisomerase I Inhibitor

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

제품 번호S2217

Irinotecan HCl Trihydrate는 Irinotecan (Camptosar, Campto, CPT-11)의 염산염 삼수화물로, LoVo 세포와 HT-29 세포에 대해 각각 15.8 및 5.17 μM의 IC50을 갖는 Topoisomerase I 억제제입니다.

Irinotecan Hydrochloride Trihydrate Topoisomerase 억제제 Chemical Structure

화학 구조

분자량: 677.18

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품질 관리

배치: 순도: 99.97%

99.97

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

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	677.18	화학식	C₃₃H₃₈N₄O₆.HCl.3H₂O	보관 (수령일로부터)	3년-20°C분말
CAS 번호	136572-09-3	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	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

용해도

In vitro
배치:

DMSO : 100 mg/mL (147.67 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL (147.67 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 5 mg/mL

Water : Insoluble

DMSO : 187.5 mg/mL (276.88 mM) 50°C 수조에서 가온; 초음파 처리;
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 5 mg/mL

Water : Insoluble

DMSO : 100 mg/mL (147.67 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 12 mg/mL

Water : 1 mg/mL

DMSO : 100 mg/mL (147.67 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	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 Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	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.

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

특징	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I
시험관 내(In vitro)	Irinotecan은 카르복실에스테라제에 의해 SN-38로 활성화되어 표적인 Topoisomerase I과 상호작용할 수 있게 됩니다. Irinotecan은 LoVo 세포 및 HT-29 세포주에서 IC50에서 유사한 양의 분리 가능한 복합체를 유도합니다. SN-38은 농도 의존적인 분리 가능한 복합체 형성을 유도하며, 이는 LoVo 세포와 HT-29 세포주에서 유의미한 차이가 없습니다. Irinotecan의 세포 축적은 현저하게 다르며, LoVo 세포보다 HT-29 세포에서 일관되게 더 높은 수준에 도달합니다. Irinotecan과 SN-38의 락톤 E-링은 수용액에서 가역적으로 가수분해되며, 락톤과 카르복실레이트 형태 간의 상호전환은 pH와 온도에 따라 달라집니다. 간은 주로 Irinotecan을 SN-38로 활성화하는 역할을 합니다. Irinotecan과 SN-38 글루쿠로나이드의 농도가 같을 때, 베타-글루쿠로니다제 매개 SN-38 생성률은 종양 및 정상 조직 모두에서 Irinotecan으로부터 형성된 것보다 높습니다. Irinotecan은 또한 장, 혈장 및 종양 조직에서 SN-38로 전환됩니다. Irinotecan은 NSCLC 세포주보다 SCLC에서 훨씬 더 활성이 높지만, SN-38에서는 조직학적 유형 간에 유의미한 차이가 관찰되지 않습니다.
생체 내(In vivo)	COLO 320 이종이식에서 Irinotecan은 최대 92%의 성장 억제를 유도합니다. 단일 용량의 Irinotecan은 위, 십이지장, 결장 및 간에서 DNA에 공유 결합된 Topoisomerase I의 양을 유의미하게 증가시킵니다. 동시에, Irinotecan 처리군은 대조군에 비해 결장 점막 세포에서 DNA 가닥 파괴의 양이 유의미하게 더 많음을 보여줍니다.
참조	[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/

적용 분야

방법	바이오마커	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

임상시험 정보

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

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
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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