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Molibresib (I-BET-762) BET remmer

Name: Molibresib (I-BET-762)
Brand: Selleck Chemicals
SKU: S7189
Rating: 5 (40 reviews)

Cat.Nr.S7189

Molibresib (I-BET-762, GSK525762, GSK525762A) is een remmer voor BET-eiwitten met een IC50 van ~35 nM in een celvrije test. Het onderdrukt de productie van pro-inflammatoire eiwitten door macrofagen en blokkeert acute ontsteking, en is zeer selectief ten opzichte van andere bromodomein-bevattende eiwitten.

Molibresib (I-BET-762) BET remmer Chemical Structure

Chemische structuur

Moleculair gewicht: 423.9

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Kwaliteitscontrole

Batch: Zuiverheid: 99.87%

99.87

Gerelateerde doelwitten	HDAC JAK Histone Methyltransferase PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Overige BET Inhibitoren	Pelabresib (CPI-0610) ZEN-3694 (BET-IN-19) Mivebresib (ABBV-075) INCB054329 Birabresib (OTX015) I-BET151 (GSK1210151A) Apabetalone (RVX-208) AZD5153 6-hydroxy-2-naphthoic acid CPI-203 I-BRD9

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving	PMID
HepG2	Function assay		18 hrs	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay, EC50 = 0.7 μM.	21568322
HepG2	Function assay		6 hrs	Induction of human ApoA1 protein synthesis in human HepG2 cells assessed as neosynthesised radiolabeled protein secretion after 6 hrs by SDS PAGE analysis in presence of [35S]methionine	21568322
HepG2	Function assay		18 hrs	Upregulation of ApoA1 expression in human HepG2 cells assessed as concentration required to increase 70% of luciferase activity after 18 hrs by luciferase reporter gene assay, EC170 = 0.2 μM.	22386529
HepG2	Function assay		18 hrs	Induction of human ApoA1 gene expression in stably transfected human HepG2 cells coexpressing luciferase reporter gene after 18 hrs by luminescence assay, EC50 = 0.7 μM.	22924434
PBMC	Antiinflammatory assay			Antiinflammatory activity against human PBMC cells assessed as LPS-induced IL-6 production by chemiluminescence assay, IC50 = 0.31623 μM.	24015967
Raji	Function assay		4 hrs	Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs, IC50 = 0.19 μM.	24900758
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0303 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0323 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0388 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0407 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0454 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0476 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0492 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0539 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki = 0.0568 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0607 μM.	26080064
MV4-11	Cytotoxicity assay		4 days	Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.093 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.0984 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.0994 μM.	26080064
Rosetta2 DE3	Function assay		30 mins	Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50 = 0.156 μM.	26080064
Rosetta2 DE3	Function assay			Binding affinity to biotinylated BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells by bio-layer interferometry method, Kd = 0.159 μM.	26080064
MOLM13	Cytotoxicity assay		4 days	Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay, IC50 = 0.241 μM.	26080064
BL21(DE3)	Function assay			Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.065 μM.	26367539
BL21(DE3)	Function assay			Binding affinity to N-terminal His6-tagged-BRD4 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.095 μM.	26367539
BL21(DE3)	Function assay			Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 2 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.1 μM.	26367539
BL21(DE3)	Function assay			Binding affinity to full length N-terminal His6-tagged-BRD2 bromodomain 1 (unknown origin) expressed in competent Escherichia coli BL21(DE3) cells by isothermal titration calorimetry, Kd = 0.23 μM.	26367539
BL21(DE3)-R3-pRARE2	Function assay			Inhibition of human His-tagged BRD4 bromodomain 2 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay, IC50 = 0.036 μM.	26731490
BL21(DE3)-R3-pRARE2	Function assay			Inhibition of human His-tagged BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3)-R3-pRARE2 cells by FRET assay, IC50 = 0.036 μM.	26731490
Rosetta2 DE3	Function assay		30 mins	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.023 μM.	28463487
Rosetta2 DE3	Function assay		30 mins	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, Ki = 0.0464 μM.	28463487
Rosetta2 DE3	Function assay		30 mins	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 2 (333 to 460 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.0775 μM.	28463487
MV4-11	Growth inhibition assay		4 days	Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay, IC50 = 0.093 μM.	28463487
Rosetta2 DE3	Function assay		30 mins	Inhibition of FAM-labeled ZBA248 binding to recombinant human N-terminal His6-tagged BRD4 bromodomain 1 (44 to 168 residues) expressed in Rosetta2 DE3 cells after 30 mins by Flourescence polarization assay, IC50 = 0.145 μM.	28463487
MOLM13	Growth inhibition assay		4 days	Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay, IC50 = 0.241 μM.	28463487
TY82	Antiproliferative assay		72 hrs	Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.2 μM.	28586718
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay, IC50 = 0.23 μM.	28586718
BL21 (DE3)-codon plus-RIL	Function assay		4 hrs	Inhibition of JQ1-FITC binding to His6-tagged BRD4-BD1 (unknown origin) expressed in Escherichia coli BL21 (DE3)-codon plus-RIL cells incubated in dark for 4 hrs by fluorescence anisotropy assay, IC50 = 0.26 μM.	28586718
THP1	Antiproliferative assay			Antiproliferative activity against human THP1 cells, IC50 = 0.29 μM.	28939121
TY82	Antiproliferative assay			Antiproliferative activity against human TY82 cells, IC50 = 0.39 μM.	28939121
NALM16	Cytotoxicity assay		5 days	Cytotoxicity against human NALM16 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 0.27 μM.	29170024
NALM6	Cytotoxicity assay		5 days	Cytotoxicity against human NALM6 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 0.39 μM.	29170024
697	Cytotoxicity assay		5 days	Cytotoxicity against human 697 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 1.17 μM.	29170024
HD-MB03	Cytotoxicity assay		5 days	Cytotoxicity against human HD-MB03 cells assessed as reduction in cell viability after 5 days by CellTiter-Glo assay, EC50 = 3.5 μM.	29170024
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
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
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 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
TY82	Antiproliferative assay		72 hrs	Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 assay, IC50 = 0.3043 μM.	29525435
MM1S	Antiproliferative assay		72 hrs	Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 assay, IC50 = 0.3492 μM.	29525435
TY82	Function assay	0.2 to 1 uM	24 hrs	Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis	29525435
TY82	Function assay	0.2 to 1 uM	24 hrs	Inhibition of BRD4 in human TY82 cells assessed as reduction in c-Myc mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis	29525435
TY82 or NCI-H1299	Function assay	0.2 to 1 uM	24 hrs	Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 protein expression at 0.2 to 1 uM after 24 hrs by Western blot analysis	29525435
TY82 or NCI-H1299	Function assay	0.2 to 1 uM	24 hrs	Inhibition of BRD4 in human TY82 or NCI-H1299 cells assessed as reduction in PD-L1 mRNA expression at 0.2 to 1 uM after 24 hrs by RT-PCR analysis	29525435
C4-2B	Antiproliferative assay		96 hrs	Antiproliferative activity against human C4-2B cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	29541371
22Rv1	Antiproliferative assay		96 hrs	Antiproliferative activity against human 22Rv1 cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	29541371
LNCAP	Antiproliferative assay		96 hrs	Antiproliferative activity against human LNCAP cells after 96 hrs by Cell-Titer glo reagent based luminescence assay	29541371
HL60	Cytotoxicity assay			Cytotoxicity against human HL60 cells by MTS assay, IC50 = 0.12 μM.	29657099
Raji	Function assay			Inhibition of BRD4-BD1 in human Raji cells assessed as downregulation of MYC gene expression by PCR method, IC50 = 0.132 μM.	29657099
LNCAP	Antiproliferative assay			Antiproliferative activity against human LNCAP cells, IC50 = 0.3565 μM.	29758518
MV411	Cytotoxicity assay		72 hrs	Cytotoxicity against human MV411 cells after 72 hrs by CellTiter-Glo assay, IC50 = 0.8 μM.	30268702
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Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	423.9	Formule	C₂₂H₂₂ClN₅O₂	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	1260907-17-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	GSK525762, GSK525762A			Smiles	CCNC(=O)CC1C2=NN=C(N2C3=C(C=C(C=C3)OC)C(=N1)C4=CC=C(C=C4)Cl)C

Oplosbaarheid

In vitro
Batch:

DMSO : 84 mg/mL (198.15 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 42 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
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	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	4.250mg/ml (10.03mM)	Taking the 1 mL working solution as an example, add 50 μL of 85 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 clarify; 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.
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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme

Targets/IC₅₀/Ki	BET proteins (Cell-free assay) 35 nM
In vitro	Molibresib (I-BET-762) is een remmer voor BET (bromodomein en extra terminale domein) eiwitten, BRD2, BRD3 en BRD4, die bindt aan de tandem bromodomeinen van BET met een K_d van 50,5-61,3 nM en een tetra-geacetyleerd H4-peptide, vooraf gebonden aan tandem bromodomeinen van BET, verdringt met een IC50 van 32,5-42,5 nM in FRET-analyse. Deze verbinding bezet de acetyl-lysine bindingsplaats van BET-eiwitten en remt hun binding aan geacetyleerde histonen, waardoor de vorming van chromatinecomplexen, essentieel voor de expressie van ontstekingsgenen, wordt verstoord. Behandeling ermee gedurende de eerste 2 dagen van differentiatie verandert de cytokineproductie van CD4⁺ T-cellen, waardoor de expressie van verschillende ontstekingsremmende genproducten wordt opgereguleerd en de expressie van verschillende pro-inflammatoire cytokines wordt neerwaarts gereguleerd.
Kinase Assay	Fluorescentie resonantie energieoverdracht (FRET) titraties
Kinase Assay	Fluorescentie resonantie energieoverdracht (FRET) titraties. Molibresib (I-BET-762) wordt getitreerd tegen BRD2 (200 nM), BRD3 (100 nM) en BRD4 (50 nM) in 50 mM HEPES pH 7,5, 50 mM NaCl, 0,5 mM CHAPS in aanwezigheid van tetra-geacetyleerd Histon H4-peptide (200 nM). Na een uur evenwicht te hebben bereikt, wordt de bromodomein-eiwit:peptide-interactie gedetecteerd met behulp van FRET na toevoeging van 2 nM Europium-cryptaat-gelabeld streptavidine en 10 nM XL-665-gelabeld anti-6His-antilichaam in testbuffer die 0,05% (v/v) BSA en 400 mM KF bevat. Platen worden gelezen met een Envision Plate-lezer (excitatie 320 nm, emissie 615 nm en 665 nm).
In vivo	Molibresib (I-BET-762) biedt bescherming tegen door lipopolysaccharide geïnduceerde endotoxische shock en door bacteriën geïnduceerde sepsis. Een enkele dosis van deze verbinding, toegediend 1,5 uur na LPS-injectie, geneest de muizen, en tweemaal daagse injecties gedurende 2 dagen beschermen hen tegen de dood veroorzaakt door sepsis. Beperkte behandeling ermee uitsluitend tijdens de vroege priming remde het vermogen van Th1-gedifferentieerde 2D2 T-cellen om neuro-inflammatie te induceren in een muismodel van experimentele auto-immune encefalomyelitis (EAE).
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/21068722/ [2] https://pubmed.ncbi.nlm.nih.gov/22912406/

Toepassingen

Methoden	Biomarkers	Afbeeldingen	PMID
Growth inhibition assay	Cell viability		26840085

Informatie klinische proef

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT03266159	Withdrawn	Solid Tumours	GlaxoSmithKline	November 27 2017	Phase 2
NCT02964507	Terminated	Neoplasms	GlaxoSmithKline	February 2 2017	Phase 1
NCT01943851	Completed	Neoplasms	GlaxoSmithKline	May 14 2014	Phase 2
NCT01587703	Completed	Carcinoma Midline	GlaxoSmithKline	March 28 2012	Phase 1

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