Topotecan HCl

別名：Nogitecan HCl, SKFS 104864A, NSC 609699

製品コード：S1231 純度：99.98%

Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively. Topotecan HCl induces autophagy and apoptosis.

CAS No. 119413-54-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 34500	国内在庫あり
50mg	JPY 27000	国内在庫あり
100mg	JPY 48000	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（53）

製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Topotecan HCl関連製品

関連ターゲット	Topo I Topo II Topo IV	もっと見る
関連製品	Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Amonafide Voreloxin (SNS-595) hydrochloride Ellagic acid Genz-644282 Hydroxy Camptothecine Rubitecan	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

Topoisomeraseシグナル伝達経路

Topoisomerase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
HeLa	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human HeLa cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
MDA-MB-231	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human MDA-MB-231 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
A375	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human A375 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
Caco2	Apoptosis assay	0.8 to 1.6 uM	24 hrs	Induction of apoptosis in human Caco2 cells assessed as inhibition of DNA synthesis at 0.8 to 1.6 uM after 24 hrs by BrdU staining-based ELISA	24980118
human MDA-MB-435 cells	Cytotoxic assay		72 h	Cytotoxicity against human MDA-MB-435 cells incubated for 72 hrs by MTT assay, GI50=34 nM	22867019
human A2780 cells	Cytotoxic assay		72 h	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=33 nM	24900725
human MOLT4 cells	Cytotoxic assay		72 h	Cytotoxicity against human MOLT4 cells after 72 hrs by MTT assay, IC50=19 nM	24900725
human LoVo cells	Cytotoxic assay		72 h	Cytotoxicity against human LoVo cells after 72 hrs by MTT assay, IC50=20 nM	20371183
human NCI-H460 cells	Proliferation assay		72 h	Antiproliferative activity against human NCI-H460 cells after 72 hrs by coulter counter analysis, IC50=16 nM	21783369
human A375 cells	Cytotoxic assay		72 h	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50=13 nM	21341674
human LNCAP cells	Cytotoxic assay		72 h	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50=9 nM	21341674
human A2780 cells	Cytotoxic assay		72 h	Cytotoxicity against human A2780 cells overexpressing alpha5beta3 integrin assessed as cell survival after 72 hrs by SRB assay, IC50=6 nM	22959246
human H69 cells	Cytotoxic assay		72 h	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50=6 nM	21341674
human A549 cells	Function assay		4 h	Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50=5 nM	18207748
human Ketr3 cells	Cytotoxic assay		96 h	Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay, IC50=4.9 nM	15165144
human MESSA cells	Cytotoxic assay		72 h	Cytotoxicity against human MESSA cells after 72 hrs by alamar blue assay, IC50=4 nM	21341674
human BGC823 cells	Cytotoxic assay		96 h	Cytotoxicity against human BGC823 cells after 96 hrs by MTT assay, IC50=4.3 nM	15165144
human A549 cells	Cytotoxic assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by MTT assay, IC50=3.2 nM	15165144
human MCF7 cells	Cytotoxic assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay, IC50=1.8 nM	15165144
human HCT8 cells	Cytotoxic assay		96 h	Cytotoxicity against human HCT8 cells after 96 hrs by MTT assay, IC50=1.5 nM	15165144
human Bel7402 cells	Cytotoxic assay		96 h	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay, IC50=1.2 nM	15165144
human MDA-MB-435 cells	Cytotoxic assay		72 h	Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay, ic50=1 nM	20371183
human U251 cells	Function assay		6-24 h	Inhibition of topoisomerase-1 in human U251 cells assessed as inhibition of hypoxia-induced HIF-1alpha accumulation in nuclear extract after 6 to 24 hrs by immunoblot analysis, EC50=54 nM	22305612
human HepG2 cells	Cytotoxic assay		4 days	Cytotoxicity against human HepG2 cells after 4 days by MTT assay, IC50=60 nM	18554906
human KB cells	Cytotoxic assay		72 h	Cytotoxicity against human KB cells after 72 hrs sulforhodamine B colorimetric assay, IC50=62.5 nM	25008456
human HCT8 cells	Cytotoxic assay		3 days	Cytotoxicity against human HCT8 cells after 3 days by MTT assay, IC50=70 nM	20392545
human GBM2 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM2 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.13 μM	26355532
SK-MEL-2 cells	Cytotoxic assay		72 h	Cytotoxicity against human SK-MEL-2 cells after 72 hrs by alamar blue assay, IC50=0.14 μM	21341674
human IGROV1 cells	Cytotoxic assay		72 h	Cytotoxicity against human IGROV1 cells after 72 hrs by alamar blue assay, IC50=0.16 μM	21341674
human U87 cells	Proliferation assay		48 h	Antiproliferative activity against human U87 cells assessed as growth inhibition after 48 hrs by MTT assay, IC50=0.16 μM	24826818
human HT1080 cells	Proliferation assay		48 h	Antiproliferative activity against human HT1080 cells assessed as growth inhibition incubated for 48 hrs by sulforhodamine B assay, IC50=0.18 μM	26408815
human Hep3B cells	Proliferation assay		72 h	Antiproliferative activity against human Hep3B cells after 72 hrs by XTT assay, GI50=0.22 μM	19796956
human GBM3 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM3 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.38 μM	26355532
human KBVIN cells	Cytotoxic assay		72 h	Cytotoxicity against human KBVIN cells after 72 hrs by SRB assay, IC50=0.4 μM	25438769
human GBM1 cells	Proliferation assay		72 h	Antiproliferative activity against human GBM1 cells assessed as reduction in cell viability incubated for 72 hrs by WST-1 method, IC50=0.46 μM	26355532
human U937 cells	Cytotoxic assay		48 h	Cytotoxicity against human U937 cells expressing p53 mutant after 48 hrs by SRB assay ， IC50=1.1 μM	19715319
Caco2	Cytotoxicity assay		24 hrs	Cytotoxicity against human Caco2 cells after 24 hrs by MTT assay, IC50=0.119μM.	24980118
Jurkat	Cytotoxicity assay		24 hrs	Cytotoxicity against human Jurkat cells after 24 hrs by MTT assay, IC50=0.127μM.	24980118
A375	Cytotoxicity assay		24 hrs	Cytotoxicity against human A375 cells after 24 hrs by MTT assay, IC50=0.162μM.	24980118
HeLa	Cytotoxicity assay		24 hrs	Cytotoxicity against human HeLa cells after 24 hrs by MTT assay, IC50=0.38μM.	24980118
MDA-MB-231	Cytotoxicity assay		24 hrs	Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50=0.473μM.	24980118
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=0.61μM.	19530720
HCT8	Antiproliferative assay		48 hrs	Antiproliferative activity against human HCT8 cells after 48 hrs by CCK8 assay, IC50=1.875μM.	25481395
KB	Antiproliferative assay		48 hrs	Antiproliferative activity against human KB cells after 48 hrs by CCK8 assay, IC50=2.282μM.	25481395
SGC7901	Antiproliferative assay		48 hrs	Antiproliferative activity against human SGC7901 cells after 48 hrs by CCK8 assay, IC50=2.292μM.	25481395
HepG2	Antiproliferative assay		48 hrs	Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay, IC50=4.208μM.	25481395
A427 human lung carcinoma	Proliferation assay			Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM	9876111
mouse P388 cells	Cytotoxic assay			Cytotoxicity against mouse P388 cells after MTT assay, IC50=45 nM	18829334
human KB3-1 cells	Cytotoxic assay			Cytotoxicity against human KB3-1 cells after MTT assay, IC50=40 nM	18829334
human stomach cancer cell line (MKN45)	Cytotoxic assay			In Vitro cytotoxicity against human stomach cancer cell line (MKN45), IC50=38 nM	11334569
human MES-SA/Dx5 cells	Cytotoxic assay			Cytotoxicity against human MES-SA/Dx5 cells overexpressing MDR1 after 72 hrs by alamar blue assay, IC50=33 nM	21341674
human lung cancer cell line (H128)	Cytotoxic assay			In Vitro cytotoxicity against human lung cancer cell line (H128), IC50=31 nM	11334569
human HCT116 cells	Growth inhibition assay			Growth inhibition of human HCT116 cells by five-dose growth inhibition assay, GI50=30 nM	25909279
UACC 62 cells	Cytotoxic assay			Tested in vitro for cytotoxicity against human tumor cell line UACC 62 (melanoma), GI50=30 nM	10714502
HeLa cells	Growth inhibition assay			Growth inhibition of HeLa cells after 4 days, GI50=30 nM	17418582
SK-BR-3 cells	Cytotoxic assay			In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3), IC50=26 nM	11334569
HT-29 cells	Cytotoxic assay			Cytotoxicity was determined in vitro in HT-29 cells(colon) of human tumor cell lines by using MTT assay, IC50=25 nM	7853331
human RPMI8226 cells	Cytotoxic assay			Cytotoxicity against human RPMI8226 cells by MTT method, IC50=21 nM	19012996
human SN12C cells	Growth inhibition assay			Growth inhibition of human SN12C cells by five-dose growth inhibition assay, GI50=20 nM	25909279
RPM18402 tumor cell line	Proliferation assay			Concentration required to inhibit cell proliferation in RPM18402 tumor cell line, IC50=20 nM	15482929
COR-L23/P cell	Cytotoxic assay			Cytotoxicity measured using the COR-L23 parental (COR-L23/P) human non small cell lung carcinoma cell line, IC50=13.2 nM	11806724
human HL60 cells	Function assay			Antitumor activity against human HL60 cells by SRB method, IC50=12 nM	19541483
LoVo cell line	Cytotoxic assay			Cytotoxic potentiation of Topotecan (TP) by the compound in (human colorectal cancer LoVo cell line, IC50=11.6 nM	12408707
human lymphoblast tumor cell line RPM18402	Cytotoxic assay			Cytotoxicity against human lymphoblast tumor cell line RPM18402, IC50=12 nM	12392745
human DU145 cells	Growth inhibition assay			Growth inhibition of human DU145 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human UACC62 cells	Growth inhibition assay			Growth inhibition of human UACC62 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human MCF7 cells	Growth inhibition assay			Growth inhibition of human MCF7 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human HOP62 cells	Growth inhibition assay			Growth inhibition of human HOP62 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
LOX cells	Cytotoxic assay			Cytotoxicity was determined in vitro in LOX cells (melanoma) of human tumor cell lines by using MTT assay, IC50=5 nM	7853331
human colon carcinoma SW620 cell	Cytotoxic assay			Cytotoxic potentiation of Topotecan (TP) by the compound in human colon carcinoma SW620 cell line, IC50=3.2 nM	12408707
human colon cancer cell line (WiDr)	Cytotoxic assay			In Vitro cytotoxicity against human colon cancer cell line (WiDr), IC50=56 nM	11334569
MDA-MB-231	Apoptosis assay			Induction of apoptosis in human MDA-MB-231 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis	24980118
A375	Apoptosis assay			Induction of apoptosis in human A375 cells assessed as p53 phosphorylation at Ser15 by Western blotting analysis	24980118
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 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
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 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
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD 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
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 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
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY 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
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 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
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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: Confirmatory screen for MG 63 (6-TG R) 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh18	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh18 cells	29435139
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 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
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: Confirmatory screen for SK-N-SH 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
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
Daoy	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for Daoy cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D caspase screen for TC32 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
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for RD cells	29435139
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生物活性

製品説明

特性

Topotecan is a water-soluble derivative of camptothecin.

Targets

Topo I (DU-145 Luc cells) ^[1] (Cell-free assay)	Topo I (MCF-7 Luc cells) ^[1] (Cell-free assay)
2 nM	13 nM

In Vitro
In vitro	Stronger drug activity of Topotecan is observed for DU-145 Luc and MCF-7 Luc cells. ^[1] Topotecan causes cytotoxicity during the course of DNA replication by stabilizing the covalent complex between topoisomerase I and DNA and preventing the religation of enzyme-linked single-strand DNA break. Topotecan stabilizes topoisomerase I/DNA cleavable complexes in radiation-resistant human B-lineage acute lymphoblastic leukemia (ALL) cells, causes rapid apoptotic cell death despite high-level expression of bcl-2 protein, and inhibits ALL cell clonogenic growth in a dose-dependent fashion. ^[2]
細胞実験	細胞株	MCF-7 Luc and DU-145 Luc cells
	濃度	0 μg/mL - 0.692 μg/mL
	反応時間	96 hours
	実験の流れ	Topotecan is dissolved in sterile water to a stock concentration of 1 mg/mL, diluted to 6 μg/mL in cultured medium and then serially diluted 1:4 in opaque, white tissue culture-treated microplates to a final volume of 0.1 mL/well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×10⁴ cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin; 100 μL of cells are added in each well. Plates are incubated for 4 days at 37 °C in 95% humidity/5% CO₂. After incubation, 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin is added to each well. After incubation at room temperature for 10 minutes, the culture microplate is measured in a microplate luminometer and a molecular light imager. Results obtained with the microplate luminometer are calculated using no inhibition control wells without exogenous drug and maximum inhibition control wells containing ATP inhibitor. Results for the molecular light imager are similarly calculated using values obtained with a 5 minutes luminescent imager.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	LC3 / p62 p53 / sesn2 / p-AMPK		23024792
	Growth inhibition assay	Cell viability		28544814

In Vivo
In Vivo	Animals inoculate s.c. with DU-145 Luc cells and then treated with Topotecan demonstrates significant tumor growth and regression as measured with calipers and luminescent imaging. The correlation coefficient is 0.75 for the control untreated group and 0.93 for the Topotecan-treated group. Similarly, tumor progression and regression are measurable using luminescent imaging for untreated and Topotecan-treated mice inoculated i.p. with MCF-7 Luc cells. ^[1] Topotecan elicited potent antileukemic activity in severe combined immune-deficiency (SCID) mouse models of human poor prognosis ALL. Topotecan markedly improved event-free survival of SCID mice challenged with otherwise fatal doses of humaln leukemia cells at systemic drug exposure levels. ^[2] Gliomas preferentially express TRAIL R2 and that treatment with Topotecan significantly up-regulates its expression. ^[3]
動物実験	動物モデル	Mice with MCF-7 Luc or DU-145 Luc cells
	投与量	0.25 mg/mL
	投与経路	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04455139	Terminated	Eye Cancer Retinoblastoma	Prof. Beck Popovic Maja\|University of Lausanne Hospitals	November 15 2021	Phase 2
NCT05083000	Unknown status	COVID-19 Respiratory Infection	National University Hospital Singapore\|Christian Medical College Vellore India	August 16 2021	Phase 1
NCT04156347	Active not recruiting	Retinoblastoma	Targeted Therapy Technologies LLC	June 16 2021	Phase 1
NCT04428879	Recruiting	Retinoblastoma	The Hospital for Sick Children	June 16 2020	Phase 1

参考
[1] Caceres G, et al. Anticancer Drugs. 2003, 14(7), 569-574. [2] Uckun FM, et al. Blood. 1995. 85(10), 2817-2828. [3] Ciusani E, et al. J Neurooncol. 2005, 71(1), 19-25. [4] McCluskey AG, et al. J Nucl Med. 2012, 53(7), 1146-1154. [5] Romanelli S, et al. Cancer Chemother Pharmacol. 1998, 41(5), 385-390. + 展開

参考

+ 展開

化学情報

分子量	457.91	化学式	C₂₃H₂₃N₃O₅.HCl
CAS No.	119413-54-6	SDF	Download Topotecan HCl SDFをダウンロードする
Smiles	CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O.Cl
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 91 mg/mL ( (198.72 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 91 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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よくある質問（FAQ）

質問1:
I would like get the compound for mice intraperitoneally injection, What would you recommend to improve solubility? What could I use as solvent (%v?) that is nontoxic (unlike Methanol) and could be injected into mice intraperitoneally?

回答
Topotecan HCl is generally prepared by Saline for I.P. administration.

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):