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Topotecan HCl inhibitor de Topoisomerase

Name: Topotecan HCl
Brand: Selleck Chemicals
SKU: S1231
Rating: 5 (58 reviews)

Réf. Catalogue: S1231

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. This compound induces autophagy and apoptosis.

Topotecan HCl Topoisomerase inhibitor Chemical Structure

Structure chimique

Poids moléculaire: 457.91

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.98%

99.98

Cibles apparentées	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Autre Topoisomerase Inhibiteurs	Camptothecin (CPT) Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Ellagic acid Amonafide Voreloxin (SNS-595) hydrochloride Hydroxy Camptothecine Cu(II)-Elesclomol 7-Ethylcamptothecin

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Description de l'activité	PMID
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 Bel7402 cells	Cytotoxic assay		96 h	Cytotoxicity against human Bel7402 cells after 96 hrs by MTT assay, IC50=1.2 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 MCF7 cells	Cytotoxic assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay, IC50=1.8 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 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 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 Ketr3 cells	Cytotoxic assay		96 h	Cytotoxicity against human Ketr3 cells after 96 hrs by MTT assay, IC50=4.9 nM	15165144
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 A549 cells	Function assay		4 h	Antitumor activity against human A549 cells after 4 hrs by MTT assay, IC50=5 nM	18207748
human H69 cells	Cytotoxic assay		72 h	Cytotoxicity against human H69 cells after 72 hrs by alamar blue assay, IC50=6 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 LNCAP cells	Cytotoxic assay		72 h	Cytotoxicity against human LNCAP cells after 72 hrs by alamar blue assay, IC50=9 nM	21341674
human HOP62 cells	Growth inhibition assay			Growth inhibition of human HOP62 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 UACC62 cells	Growth inhibition assay			Growth inhibition of human UACC62 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
human DU145 cells	Growth inhibition assay			Growth inhibition of human DU145 cells by five-dose growth inhibition assay, IC50=10 nM	25909279
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 HL60 cells	Function assay			Antitumor activity against human HL60 cells by SRB method, IC50=12 nM	19541483
human A375 cells	Cytotoxic assay		72 h	Cytotoxicity against human A375 cells after 72 hrs by alamar blue assay, IC50=13 nM	21341674
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 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 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
RPM18402 tumor cell line	Proliferation assay			Concentration required to inhibit cell proliferation in RPM18402 tumor cell line, IC50=20 nM	15482929
human SN12C cells	Growth inhibition assay			Growth inhibition of human SN12C cells by five-dose growth inhibition assay, GI50=20 nM	25909279
human RPMI8226 cells	Cytotoxic assay			Cytotoxicity against human RPMI8226 cells by MTT method, IC50=21 nM	19012996
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
SK-BR-3 cells	Cytotoxic assay			In Vitro cytotoxicity against human breast cancer cell line (SK-BR-3), IC50=26 nM	11334569
HeLa cells	Growth inhibition assay			Growth inhibition of HeLa cells after 4 days, GI50=30 nM	17418582
UACC 62 cells	Cytotoxic assay			Tested in vitro for cytotoxicity against human tumor cell line UACC 62 (melanoma), GI50=30 nM	10714502
human HCT116 cells	Growth inhibition assay			Growth inhibition of human HCT116 cells by five-dose growth inhibition assay, GI50=30 nM	25909279
human lung cancer cell line (H128)	Cytotoxic assay			In Vitro cytotoxicity against human lung cancer cell line (H128), IC50=31 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 A2780 cells	Cytotoxic assay		72 h	Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, IC50=33 nM	24900725
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 stomach cancer cell line (MKN45)	Cytotoxic assay			In Vitro cytotoxicity against human stomach cancer cell line (MKN45), IC50=38 nM	11334569
human KB3-1 cells	Cytotoxic assay			Cytotoxicity against human KB3-1 cells after MTT assay, IC50=40 nM	18829334
mouse P388 cells	Cytotoxic assay			Cytotoxicity against mouse P388 cells after MTT assay, IC50=45 nM	18829334
A427 human lung carcinoma	Proliferation assay			Antiproliferative activity measured against A427 human lung carcinoma, IC50=49 nM	9876111
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 colon cancer cell line (WiDr)	Cytotoxic assay			In Vitro cytotoxicity against human colon cancer cell line (WiDr), IC50=56 nM	11334569
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
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
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
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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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	457.91	Formule	C₂₃H₂₃N₃O₅.HCl	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	119413-54-6	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	Nogitecan HCl, SKFS 104864A, NSC 609699			Smiles	CCC1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O.Cl

Solubilité (Solubility)

In vitro
Lot:

DMSO : 91 mg/mL (198.72 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : 91 mg/mL

Ethanol : 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.
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	Saline Validé par les laboratoires Selleck. Si vous avez besoin d'ajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	30.000mg/ml (65.52mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

Calculateur de formulation in vivo (Solution claire)

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

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

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y 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 d'abord 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 d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout 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 d'action (Mechanism of Action)

Caractéristiques	Topotecan is a water-soluble derivative of camptothecin.
Targets/IC₅₀/Ki	Topo I (DU-145 Luc cells) (Cell-free assay) 2 nM Topo I (MCF-7 Luc cells) (Cell-free assay) 13 nM
In vitro	Une activité médicamenteuse plus forte de Topotecan HCl est observée pour les cellules DU-145 Luc et MCF-7 Luc. Ce composé provoque une cytotoxicité pendant la réplication de l'ADN en stabilisant le complexe covalent entre la topoisomerase I et l'ADN et en empêchant la religature de la cassure de l'ADN simple brin liée à l'enzyme. Il stabilise les complexes clivables topoisomerase I/ADN dans les cellules de leucémie aiguë lymphoblastique (ALL) de lignée B humaine résistantes aux radiations, provoque une mort cellulaire apoptotique rapide malgré une expression de haut niveau de la protéine bcl-2, et inhibe la croissance clonogénique des cellules ALL de manière dose-dépendante.
In vivo	Les animaux inoculés par voie sous-cutanée avec des cellules DU-145 Luc et ensuite traités avec Topotecan HCl montrent une croissance et une régression tumorales significatives mesurées à l'aide de pieds à coulisse et d'imagerie luminescente. Le coefficient de corrélation est de 0,75 pour le groupe témoin non traité et de 0,93 pour le groupe traité par ce composé. De même, la progression et la régression tumorales sont mesurables à l'aide de l'imagerie luminescente pour les souris non traitées et traitées par ce produit chimique inoculées par voie intrapéritonéale avec des cellules MCF-7 Luc. Ce composé a exercé une puissante activité antileucémique dans des modèles murins de déficit immunitaire combiné sévère (SCID) de leucémie aiguë lymphoblastique (ALL) humaine à pronostic défavorable. Il a considérablement amélioré la survie sans événement des souris SCID exposées à des doses autrement fatales de cellules leucémiques humaines à des niveaux d'exposition systémique au médicament. Les gliomes expriment préférentiellement TRAIL R2 et le traitement avec ce produit chimique régule significativement son expression à la hausse.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/12960742/ [2] https://pubmed.ncbi.nlm.nih.gov/7742543/ [3] https://pubmed.ncbi.nlm.nih.gov/15719269/ [4] https://pubmed.ncbi.nlm.nih.gov/22689924/ [5] https://pubmed.ncbi.nlm.nih.gov/9523734/

Applications (Applications)

Méthodes	Biomarqueurs	Images	PMID
Western blot	LC3 / p62 p53 / sesn2 / p-AMPK		23024792
Growth inhibition assay	Cell viability		28544814

Informations sur l'essai clinique (Clinical Trial Information)

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

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
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

Foire aux questions (Frequently Asked Questions)

Question 1:
I would like to get it 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?

Réponse :
It 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):