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Cabozantinib (XL184) inhibiteur de Met/VEGFR2

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

Réf. CatalogueS1119

Puissant inhibiteur de VEGFR2 avec une IC50 de 0,035 nM, le Cabozantinib (XL184) inhibe également c-Met, Ret, Kit, Flt-1/3/4, Tie2 et AXL avec une IC50 de 1,3 nM, 4 nM, 4,6 nM, 12 nM/11,3 nM/6 nM, 14,3 nM et 7 nM dans des essais sans cellules, respectivement. Il induit une apoptose dépendante de PUMA dans les cellules de cancer du côlon via la voie de signalisation AKT/GSK-3β/NF-κB.

Cabozantinib (XL184) VEGFR Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 501.51

Aller à

Contrôle Qualité (Quality Control)

Lot : Pureté : 99.99%

99.99

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

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

Lignées cellulaires	Type d'essai	Concentration	Temps d'incubation	Formulation	Description de l'activité	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
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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire	501.51	Formule	C₂₈H₂₄FN₃O₅	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	849217-68-1	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	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

Solubilité (Solubility)

In vitro
Lot:

DMSO : 100 mg/mL (199.39 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

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.

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)

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) a une faible activité inhibitrice contre RON et PDGFRβ avec une IC50 de 124 nM et 234 nM, respectivement, et a une faible activité contre FGFR1 avec une IC50 de 5,294 μM. À faible concentration (0,1-0,5 μM), il est suffisant pour induire une inhibition marquée de la phosphorylation constitutive et inductible de Met et de sa signalisation en aval résultante dans les cellules MPNST, et pour inhiber la migration et l'invasion des cellules MPNST induites par le HGF. Ce composé induit également une inhibition marquée de la phosphorylation de Met et VEGFR2 dans les cellules endothéliales de la veine ombilicale humaine (HUVECs) stimulées par les cytokines. Bien qu'il n'ait pas d'effet significatif sur la croissance des cellules MPNST à 0,1 μM, XL184 à 5-10 μM inhibe significativement la croissance des cellules MPNST.
In vivo	Le traitement au Cabozantinib (XL184) à 30 mg/kg chez des souris RIP-Tag2 avec des tumeurs spontanées des îlots pancréatiques perturbe 83 % de la vascularisation tumorale, réduit les péricytes et les manchons de membrane basale vides, provoque une hypoxie intratumorale généralisée et une apoptose étendue des cellules tumorales, et ralentit la repousse de la vascularisation tumorale après le retrait du médicament, de manière plus significative par rapport au XL999 qui bloque VEGFR mais pas c-Met, ce qui entraîne seulement une réduction de 43 % de la vascularisation, suggérant qu'une inhibition concurrente de VEGFR et d'autres récepteurs tyrosine kinases (RTK) fonctionnellement pertinents amplifie l'inhibition de l'angiogenèse. Ce composé diminue également l'invasivité des tumeurs primaires et réduit les métastases. À 30 mg/kg/jour, il abroge significativement la croissance et la métastase des xénogreffes de MPNST humaines chez les souris SCID. L'administration de XL184 induit une inhibition dose-dépendante de la croissance tumorale dans des modèles de tumeurs du sein, du poumon et du gliome, en association avec une diminution de la prolifération des cellules tumorales et endothéliales ainsi qu'une augmentation de l'apoptose. Une dose orale unique est suffisante pour induire une inhibition soutenue de la croissance tumorale chez les souris porteuses de tumeurs MDA-MB-231 et les rats porteurs de tumeurs C6 à 100 mg/kg et 10 mg/kg, respectivement.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/21613405/ [2] https://pubmed.ncbi.nlm.nih.gov/21540237/ [3] https://pubmed.ncbi.nlm.nih.gov/21926191/

Applications (Applications)

Méthodes	Biomarqueurs	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

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
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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C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
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