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Regorafenib (BAY 73-4506) Inhibiteur de multikinases

Name: Regorafenib (BAY 73-4506)
Brand: Selleck Chemicals
SKU: S1178
Rating: 5 (216 reviews)

Réf. CatalogueS1178

Regorafenib est un inhibiteur multi-cibles pour VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) et Raf-1 avec des IC50 de 13 nM/4,2 nM/46 nM, 22 nM, 7 nM, 1,5 nM et 2,5 nM dans des essais sans cellules, respectivement. Regorafenib induit l'Autophagy.

Regorafenib (BAY 73-4506) VEGFR inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 482.82

Aller à

Contrôle Qualité

Lot : Pureté : 99.91%

99.91

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 ZM 323881 HCl

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Concentration	Temps dincubation	Formulation	Description de lactivité	PMID
Hep3B	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
PLC/PRF/5	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HepG2	Apoptosis Assay	1–5 μM	48 h		inhibits cell growth	26329608
HEK293	Function Assay	0.5 μM	2/4/6 h		reduces GRP78 expression	25858032
GEO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HT29	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW480	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW620	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT116	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
LOVO	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
HCT150	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
SW48-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
GEO-CR	Growth Inhibition Assay	0.01-20 μM	96 h	DMSO	inhibits cell growth in a dose-dependent manner	25838391
KB-31	Growth Inhibition Assay				IC50=5.5±0.3 nM	25753361
KB-G2	Growth Inhibition Assay				IC50=9.1±0.1 nM	25753361
LLC-PK1	Growth Inhibition Assay				IC50=42.0±3.2 nM	25753361
LLC-PK1/MRP2	Growth Inhibition Assay				IC50=82.4±2.7 nM	25753361
HEK293	Growth Inhibition Assay				IC50=11.0±1.2 nM	25753361
HEK293/OATP1B1	Growth Inhibition Assay				IC50=6.2±0.3 nM	25753361
HROC18	Growth Inhibition Assay				IC50=1.3 μM	25309914
HROC24	Growth Inhibition Assay				IC50=4.6 μM	25309914
HROC43	Growth Inhibition Assay				IC50=5.3 μM	25309914
HROC46	Growth Inhibition Assay				IC50=2.4 μM	25309914
RJ345	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
RJ348	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MCF-7	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
MDA-MB-231	Function Assay	0.5/5 μM	24 h	DMSO	inhibits the cell migration	25253994
HT15	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
DLD1	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT-29	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
Hct-116	Growth Inhibition Assay	1-20 μM	48 h		inhibits cell growth in a dose-dependent manner	25071018
HT15	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
DLD1	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
HT-29	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
Hct-116	Apoptosis Assay	1-10 μM	48 h		induces cell death in a dose-dependent manner	25071018
GBM5	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM6	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM12	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
GBM14	Apoptosis Assay	0.5–1.0 μM	24 h	DMSO	interacts with lapatinib to induce cell death	24911215
Hep3B	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
PLC/PRF/5	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HepG2	Growth Inhibition Assay	1–2.5 μM	24/48/72 h		inhibits cell growth	24885890
HCT116	Function Assay	10/20/40 μM	24 h		induces PUMA protein and mRNA expression in a dose- and time-dependent manner	24763611
Lim2405	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
LoVo	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Lim1215	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW48	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
RKO	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW837	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW1463	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
SW480	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco432	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
Vaco400	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
DLD1	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
HT29	Function Assay	40 μM	24 h		induces PUMA protein and cell apoptosis	24763611
PLC/PRF/5	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
HepG2	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
Hep3B	Growth Inhibition Assay	1–5µM	24/48/72 h		inhibits cell growth	23169148
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.021 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.047 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.049 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.051 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.063 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.094 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.108 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.13 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.231 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.29 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.38 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.522 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.549 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.833 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.834 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.943 μM.	30204441
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.27 μM.	30204441
GISTT1	Cytotoxicity assay		72 hrs		Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.35 μM.	28991465
BA/F3	Growth inhibition assay		72 hrs		Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.371 μM.	30204441
GIST430	Cytotoxicity assay		72 hrs		Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 3 μM.	28991465
BA/F3	Cytotoxicity assay		72 hrs		Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 9.953 μM.	30204441
U-2 OS	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells	29435139
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
BT-12	qHTS assay				qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 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
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
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Informations chimiques, stockage et stabilité

Poids moléculaire	482.82	Formule	C₂₁H₁₅ClF₄N₄O₃	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	755037-03-7	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	Fluoro-Sorafenib, BAY 73-4506			Smiles	CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F

Solubilité

In vitro
Lot:

DMSO : 97 mg/mL (200.9 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Ethanol : 3 mg/mL

Water : 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.
Clear solution	2% DMSO 1 30% PEG 300 2 5% Tween 80 3 ddH2O Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 300 μL PEG300, mix evenly to clarify it; add 50 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 630 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	2%DMSO 1 98% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 20 μL of 250 mg/ml clarified DMSO stock solution to 980 μL of corn oil and mix evenly. 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.
Clear solution	5%DMSO 1 95% Corn oil Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	5.000mg/ml (10.36mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 950 μL of corn oil and mix evenly. 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.
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 lexpérience)

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

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny 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 dabord 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 dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout 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 daction

Targets/IC₅₀/Ki	RET (Cell-free assay) 1.5 nM Raf-1 (Cell-free assay) 2.5 nM VEGFR2 (Cell-free assay) 4.2 nM Kit (Cell-free assay) 7 nM VEGFR1 (Cell-free assay) 13 nM B-Raf (V600E) (Cell-free assay) 19 nM PDGFRβ (Cell-free assay) 22 nM B-Raf (Cell-free assay) 28 nM VEGFR3 (Cell-free assay) 46 nM
In vitro	Regorafenib prévient fortement l'autophosphorylation de VEGFR2 dans les cellules NIH-3T3/VEGFR2 avec une IC50 de 3 nM. Dans les HAoSMCs, ce composé supprime l'autophosphorylation de PDGFR-β après stimulation par le PDGF-BB, avec une IC50 de 90 nM. Il inhibe également la signalisation de FGFR dans les cellules de cancer du sein (BC) MCF-7 stimulées par le FGF10. Cette substance chimique a très puissamment inhibé les récepteurs mutants KIT^K642E et RET^C634W, avec des IC50 d'environ 20 nM et 10 nM, respectivement. Il inhibe la prolifération des HUVECs stimulées par le VEGF¹⁶⁵, avec une IC50 d'environ 3 nM. Ce composé prévient la prolifération des HUVECs stimulées par le FGF2 et des HAoSMCs stimulées par le PDGF-BB avec des IC50 de 127 nM et 146 nM, respectivement. Il cible à la fois la prolifération des cellules tumorales et la vascularisation tumorale par l'inhibition des récepteurs des Protein Tyrosine Kinase (VEGFR, KIT, RET, FGFR et PDGFR) et des sérine/thréonine kinases (Raf et p38MAPK). Cette substance chimique supprime la croissance des cellules humaines Hep3B, PLC/PRF/5 et HepG2 de manière dépendante de la concentration et du temps.
Essai kinase	Essais kinases
Essai kinase	Des essais in vitro utilisant les domaines kinase recombinants de VEGFR2 (murin aa785–aa1367), VEGFR3 (murin aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) et BRafV600E (aa409–aa765) sont réalisés. Le profilage initial d'inhibition de kinase in vitro est effectué à une concentration fixe de 1 μM de ce composé. Les valeurs de concentration inhibitrice de 50% (IC50) sont déterminées à partir des kinases répondantes sélectionnées, par exemple, VEGFR1 et RET. L'inhibition de la kinase TIE2 est mesurée avec un essai de fluorescence homogène résolue dans le temps (HTRF) utilisant une protéine de fusion recombinante de glutathion-S-transférase, le domaine intracellulaire de TIE2 et le peptide biotine-Ahx-EPKDDAYPLYSDFG comme substrat.
In vivo	Regorafenib révèle un TGI puissant et dose-dépendant dans divers modèles précliniques de xénogreffes humaines chez la souris, avec des régressions tumorales dans les modèles de carcinome mammaire MDA-MB-231 et rénal 786-O. Ce composé prévient non seulement la croissance des tumeurs primaires syngéniques du sein 4T1 poussant orthotopiquement dans le coussinet adipeux, mais supprime également la formation de métastases tumorales dans le poumon.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/21170960/ [2] https://pubmed.ncbi.nlm.nih.gov/21789125/ [3] https://pubmed.ncbi.nlm.nih.gov/22777740/

Applications

Méthodes	Biomarqueurs	PMID
Western blot	p-STAT3 / STAT3 / PARP / Caspase-9 Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK p-p65(S536) / p65 Bim / Bid / Bak / Bcl-Xl / Mcl-1 PUMA / p53	25071018
Immunofluorescence	F-actin / Vimentin / E-cadherin p65	27580057
Growth inhibition assay	Cell viability GI50	25071018

Informations sur lessai clinique

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

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT06321055	Not yet recruiting	Advanced Gastrointestinal Stromal Tumor	Bayer	March 20 2024	--
NCT06137170	Active not recruiting	Metastatic Colorectal Cancer	Bayer	March 1 2024	--
NCT06029010	Completed	Metastatic Colorectal Cancer	Bayer	August 31 2023	--
NCT05370807	Recruiting	Melanoma Stage III\|Melanoma Stage IV	Universitair Ziekenhuis Brussel	October 3 2022	Phase 2

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

Foire aux questions

Question 1:
How to resuspend it for in vivo studies?

Réponse :
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml for it.

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):