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Cabozantinib (XL184) Met/VEGFR2-remmer

Name: Cabozantinib (XL184)
Brand: Selleck Chemicals
SKU: S1119
Rating: 5 (168 reviews)

Cat.nr.S1119

Een potente VEGFR2-remmer met een IC50 van 0,035 nM, Cabozantinib (XL184) remt ook c-Met, Ret, Kit, Flt-1/3/4, Tie2 en AXL met een IC50 van respectievelijk 1,3 nM, 4 nM, 4,6 nM, 12 nM/11,3 nM/6 nM, 14,3 nM en 7 nM in celvrije assays. Het induceert PUMA-afhankelijke apoptosis in darmkankercellen via de AKT/GSK-3β/NF-κB-signaalroute.

Cabozantinib (XL184) VEGFR Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 501.51

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	EGFR PDGFR FGFR c-Met Src MEK CSF-1R FLT3 HER2 c-Kit
Overig VEGFR Inhibitoren	SAR131675 SU 5402 Cediranib (AZD2171) Vatalanib (PTK787) 2HCl Anlotinib (AL3818) Dihydrochloride Linifanib (ABT-869) Apatinib (YN968D1) Apatinib (YN968D1) mesylate Ki8751 Semaxanib (SU5416)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
E98NT	Growth Inhibition Assay	0.01-10 μM		DMSO	IC50=89 nM	23484006
SNU-5	Growth Inhibition Assay				IC50= 19 nM	21926191
Hs746T	Growth Inhibition Assay				IC50=9.9 nM	21926191
SNU-1	Growth Inhibition Assay				IC50=5223 nM	21926191
SNU-16	Growth Inhibition Assay				IC50=1149 nM	21926191
MDA-MB-231	Growth Inhibition Assay				IC50= 6421 nM	21926191
U87MG	Growth Inhibition Assay				IC50=1851 nM	21926191
H441	Growth Inhibition Assay				IC50=21700 nM	21926191
H69	Growth Inhibition Assay				IC50=20200 nM	21926191
PC3	Growth Inhibition Assay				IC50=10800 nM	21926191
MTC-TT	Growth Inhibition Assay				IC50=0.04 + 0.03 μM	21470995
MZ-CRC	Growth Inhibition Assay				IC50> 5 μM	21470995
TPC-1	Growth Inhibition Assay				IC50=0.06 + 0.02 μM	21470995
NIH-3T3/TPR-Met	Function assay				Inhibition of cell proliferation in mouse NIH-3T3/TPR-Met cells, IC50 = 1 μM.	24996144
BA/F3	Growth inhibition assay				Inhibition of TEL-fused VEGFR2 (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition, GI50 = 0.003 μM.	26652860
BaF3	Growth inhibition assay		48 hrs		Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.01 μM.	26652860
BA/F3	Growth inhibition assay		48 hrs		Inhibition of wild type TEL-fused RET (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.05 μM.	26652860
TT	Growth inhibition assay		10 days		Inhibition of RET C634W mutant in human TT cells assessed as cell growth inhibition after 10 days by MTT assay, GI50 = 0.12 μM.	26652860
BA/F3	Growth inhibition assay		48 hrs		Inhibition of TEL-fused Ret V804M mutant (unknown origin) expressed in mouse BA/F3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.89 μM.	26652860
BaF3	Growth inhibition assay		48 hrs		Inhibition of TEL-fused Ret V804L mutant (unknown origin) expressed in mouse BaF3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, GI50 = 0.91 μM.	26652860
Nthy-ori 3-1	Cytotoxicity assay		10 days		Cytotoxicity against human Nthy-ori 3-1 cells after 10 days by MTT assay, GI50 = 4.93 μM.	26652860
BAF3	Function assay	0.01 to 10 uM	1 hr		Inhibition of TEL-fused wild type Ret (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis	26652860
TT	Function assay		4 hrs		Inhibition of autophosphorylation of RET C634W mutant at Y905 in human TT cells at 1 uM after 4 hrs by Western blot analysis	26652860
BAF3	Function assay	0.01 to 10 uM	1 hr		Inhibition of TEL-fused Ret S891A mutant (unknown origin) phosphorylation at Y1062/Y905 expressed in mouse BAF3 cells at 0.01 to 10 uM after 1 hr by Western blot analysis	26652860
BAF3	Function assay	0.01 to 10 uM	1 hr		Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of PLCgamma at Y783 at 0.01 to 10 uM after 1 hr by Western blot analysis	26652860
BAF3	Function assay	0.01 to 10 uM	1 hr		Inhibition of TEL-fused Ret S891A mutant (unknown origin) expressed in mouse BAF3 cells assessed as suppression of phosphorylation of Shc at Y317 at 0.01 to 10 uM after 1 hr by Western blot analysis	26652860
TT	Function assay	1 to 10 uM	4 hrs		Inhibition of RET C634W mutant in human TT cells assessed as suppression of PLCgamma phosphorylation at Y783 at 1 to 10 uM after 4 hrs by Western blot analysis	26652860
TT	Function assay	1 to 10 uM	4 hrs		Inhibition of RET C634W mutant in human TT cells assessed as suppression of ERK phosphorylation at T202/Y204 at 1 to 10 uM after 4 hrs by Western blot analysis	26652860
TT	Function assay	1 to 10 uM	4 hrs		Inhibition of RET C634W mutant in human TT cells assessed as suppression of AKT phosphorylation at T308/S473 at 1 to 10 uM after 4 hrs by Western blot analysis	26652860
TT	Function assay	1 uM			Inhibition of Ret-driven oncogenic transformation of human TT cells at 1 uM by soft agar assay	26652860
TT	Function assay	1 uM	4 hrs		Inhibition of autophosphorylation of RET C634W mutant at Y1062 in human TT cells at 1 uM after 4 hrs by Western blot analysis	26652860
TT	Apoptosis assay	1 uM	96 hrs		Induction of apoptosis in human TT cells expressing Ret C634W mutant at 1 uM after 96 hrs by annexinV/PI staining-based flow cytometric analysis	26652860
PC3	Function assay		1 to 3 hrs		Inhibition of c-Met phosphorylation in human PC3 cells incubated for 1 to 3 hrs, IC50 = 1.9 μM.	26717201
MDA-MB-231	Function assay		1 to 3 hrs		Inhibition of AXL phosphorylation in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 5 μM.	26717201
BAF3	Function assay		1 to 3 hrs		Inhibition of FLT3 (unknown origin) phosphorylation transfected in mouse BAF3 cells incubated for 1 to 3 hrs, IC50 = 7.5 μM.	26717201
MDA-MB-231	Function assay		1 to 3 hrs		Inhibition of KIT (unknown origin) phosphorylation transfected in human MDA-MB-231 cells incubated for 1 to 3 hrs, IC50 = 42 μM.	26717201
BA/F3	Function assay		48 hrs		Inhibition of KDR (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.014 μM.	26874741
Sf21	Function assay		15 mins		Inhibition of recombinant His-tagged human KDR expressed in insect Sf21 cells preincubated for 15 mins followed by substrate addition measured after 20 mins by HTRF assay, IC50 = 0.016 μM.	26874741
BA/F3	Function assay		48 hrs		Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM.	26874741
BA/F3	Function assay		48 hrs		Inhibition of KIF5B/RET (unknown origin) expressed in mouse BA/F3 cells assessed as reduction in cell viability after 48 hrs by Cell titre glo-based luminescence assay, IC50 = 0.19 μM.	26874741
BA/F3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay, IC50 = 0.0219 μM.	27068889
Sf21	Function assay		60 mins		Inhibition of wild type N-terminal GST-tagged recombinant human RET (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.003 μM.	27131066
Sf21	Function assay		60 mins		Inhibition of N-terminal GST-tagged recombinant human RET V804M mutant (658 residues) expressed in insect Sf21 cells using poly(Glu,Tyr)4:1 as substrate incubated for 60 mins by ELISA, IC50 = 0.811 μM.	27131066
BaF3	Function assay		72 hrs		Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM.	27131066
BaF3	Function assay		72 hrs		Inhibition of CCDC6-RET (unknown origin) expressed in mouse BaF3 cells assessed as inhibition of cell proliferation after 72 hrs by SRB/CCK-8 assay, IC50 = 0.889 μM.	27131066
Ba/F3	Function assay				Inhibition of RET (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.07 μM.	27814560
TT	Function assay				Inhibition of RET C634W mutant in human TT cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.26 μM.	27814560
Ba/F3	Function assay				Inhibition of RET V804M mutant (unknown origin) transfected in mouse Ba/F3 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 0.74 μM.	27814560
Nthy-ori 3-1	Cytotoxicity assay				Cytotoxicity against human Nthy-ori 3-1 cells assessed as reduction in cell viability by CellTiter-Glo luminescence assay, GI50 = 2.92 μM.	27814560
HepG2	Antiproliferative assay		72 hrs		Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay, IC50 = 0.012 μM.	28412159
EBC1	Antiproliferative assay		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0514 μM.	28412159
H1299	Growth inhibition assay		72 hrs		Growth inhibition of human H1299 cells incubated for 72 hrs by CCK8 assay, IC50 = 1.919 μM.	28651979
MCF7	Growth inhibition assay		72 hrs		Growth inhibition of human MCF7 cells incubated for 72 hrs by CCK8 assay, IC50 = 2.889 μM.	28651979
A549	Growth inhibition assay		72 hrs		Growth inhibition of human A549 cells incubated for 72 hrs by CCK8 assay, IC50 = 4.205 μM.	28651979
T47D	Growth inhibition assay		72 hrs		Growth inhibition of human T47D cells incubated for 72 hrs by CCK8 assay, IC50 = 4.448 μM.	28651979
H460	Growth inhibition assay		72 hrs		Growth inhibition of human H460 cells incubated for 72 hrs by CCK8 assay, IC50 = 5.669 μM.	28651979
HuH7	Antiproliferative assay		48 hrs		Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay, IC50 = 4.348 μM.	29057042
A498	Antiproliferative assay		48 hrs		Antiproliferative activity against human A498 cells after 48 hrs by MTT assay, IC50 = 8.456 μM.	29057042
NCI-H727	Antiproliferative assay		48 hrs		Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay, IC50 = 14.01 μM.	29057042
BAF3	Antiproliferative assay		72 hrs		Antiproliferative activity against mouse BAF3 cells harboring TRP-MET after 72 hrs by CCK-8 assay, IC50 = 0.024 μM.	29146452
A549	Cytotoxicity assay	10 uM	72 hrs		Cytotoxicity against human A549 cells at 10 uM after 72 hrs by Incucyte live-cell imaging analysis	29407963
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
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
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
A673	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 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
OHS-50	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
Rh41	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory 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
Rh18	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 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
TC32	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 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
EBC1	Antiproliferative assay		72 hrs		Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay, IC50 = 0.0048 μM.	30248654
MKN45	Antiproliferative assay		72 hrs		Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay, IC50 = 0.0069 μM.	30248654
SNU5	Antiproliferative assay		72 hrs		Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay, IC50 = 0.0121 μM.	30248654
BAF3	Function assay		72 hrs		Inhibition of TPR-tagged met (unknown origin) expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay, IC50 = 0.01986 μM.	30248654
NCI-H460	Antiproliferative assay		72 hrs		Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50 = 0.0401 μM.	30248654
MGHU3	Antiproliferative assay		72 hrs		Antiproliferative activity against human MGHU3 cells after 72 hrs by CellTiter-Glo assay	30309671
RT112	Antiproliferative assay		72 hrs		Antiproliferative activity against human RT112 cells after 72 hrs by CellTiter-Glo assay	30309671
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	501.51	Formule	C₂₈H₂₄FN₃O₅	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	849217-68-1	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	BMS-907351			Smiles	COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (199.39 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
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Verdunningscalculator Molecuulgewichtcalculator

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.
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 formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met 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 de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

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

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Targets/IC₅₀/Ki	VEGFR2/KDR (Cell-free assay) 0.035 nM c-Met (Cell-free assay) 1.3 nM Axl (Cell-free assay) 7 nM
In vitro	Cabozantinib (XL184) heeft een zwakke remmende activiteit tegen RON en PDGFRβ met IC50 van respectievelijk 124 nM en 234 nM, en heeft een lage activiteit tegen FGFR1 met IC50 van 5,294 μM. Bij lage concentratie (0,1-0,5 μM) is het voldoende om een duidelijke remming te induceren van constitutieve en induceerbare Met-fosforylatie en de daaruit voortvloeiende downstream-signalering in MPNST-cellen, en om HGF-geïnduceerde MPNST-celmigratie en -invasie te remmen. Deze verbinding induceert ook een duidelijke remming van Met- en VEGFR2-fosforylatie in cytokine-gestimuleerde menselijke navelstrengendotheelcellen (HUVEC's). Hoewel het geen significant effect heeft op de MPNST-celgroei bij 0,1 μM, remt XL184 bij 5-10 μM de MPNST-celgroei significant.
In vivo	Cabozantinib (XL184) behandeling met 30 mg/kg in RIP-Tag2-muizen met spontane pancreatische eilandjestumoren verstoort 83% van de tumorvascularisatie, vermindert pericyten en lege basaalmembraanhoezen, veroorzaakt wijdverspreide intratumorale hypoxie en uitgebreide tumorcelapoptose, en vertraagt de hergroei van de tumorvascularisatie na medicatieonderbreking, significant meer vergeleken met XL999 dat VEGFR maar niet c-Met blokkeert, wat leidt tot slechts 43% vermindering van de vascularisatie, wat suggereert dat gelijktijdige remming van VEGFR en andere functioneel relevante receptor tyrosinekinasen (RTK) de angiogenese-remming versterkt. Deze verbinding vermindert ook de invasiviteit van primaire tumoren en vermindert metastase. Bij 30 mg/kg/dag, onderdrukt het significant de groei en metastase van humane MPNST-xenografts in SCID-muizen. Toediening van XL184 induceert dosisafhankelijke remming van tumorgroei in borst-, long- en glioomtumormodellen, in samenhang met verminderde tumor- en endotheelcelproliferatie en verhoogde apoptose. Een enkele orale dosis is voldoende om aanhoudende tumorgroei-remming te induceren in MDA-MB-231 tumor-dragende muizen en C6 tumor-dragende ratten bij respectievelijk 100 mg/kg en 10 mg/kg.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/21613405/ [2] https://pubmed.ncbi.nlm.nih.gov/21540237/ [3] https://pubmed.ncbi.nlm.nih.gov/21926191/

Toepassingen (Applications)

Methoden	Biomarkers	PMID
Western blot	p-MET / p-ERK / p-AKT p-MET(Y1234/1235) / MET / p-EGFR(Y1068) / EGFR / p-Gab1(Y627) / Gab1 / p-AKT(S473) / p-ERK / p-EIF4E	29520051
Immunofluorescence	α-tubulin	29520051
Growth inhibition assay	Cell viability	23661005

Informatie over klinische proeven (Clinical Trial Information)

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

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT06156410	Recruiting	Ewing Sarcoma\|Osteosarcoma	Children''s Hospital of Philadelphia\|Children''s Hospital Colorado\|Exelixis\|Alex''s Lemonade Stand Foundation	October 24 2023	Phase 1
NCT05249114	Active not recruiting	Neuroendocrine Tumors	Providence Health & Services\|Exelixis\|Advanced Accelerator Applications SA	December 28 2022	Phase 1
NCT05444933	Completed	Advanced Renal Cell Carcinoma	Ipsen	September 16 2022	--

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