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Regorafenib (BAY 73-4506) Multikinase inhibitor

Name: Regorafenib (BAY 73-4506)
Brand: Selleck Chemicals
SKU: S1178
Rating: 5 (217 reviews)

Kat.-Nr.: S1178

Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy.

Regorafenib (BAY 73-4506) VEGFR inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 482.82

Springe zu

Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.91%

99.91

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

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Formulierung	Aktivitätsbeschreibung	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
Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht	482.82	Formel	C₂₁H₁₅ClF₄N₄O₃	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	755037-03-7	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 97 mg/mL (200.9 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble

DMSO : 96 mg/mL (198.83 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 97 mg/mL (200.9 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molaritätsrechner

Masse	Konzentration	Volumen	Molekulargewicht
=	×	×

Verdünnungsrechner Molekulargewichtsrechner

In vivo Charge:
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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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 Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	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.

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH₂O, mischen und klären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.

Wirkmechanismus (Mechanism of Action)

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 strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, this compound suppresses PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. It also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. This chemical very potently inhibited the mutant receptors KIT^K642E and RET^C634W, with IC50 of approximately 20 nM and 10 nM, respectively. It inhibits the proliferation of VEGF¹⁶⁵-stimulated HUVECs, with an IC50 of approximately 3 nM. This compound prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. It targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). This chemical suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner.
Kinase-Assay	Kinase-Assays
Kinase-Assay	In-vitro-Assays unter Verwendung rekombinanter VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) und BRafV600E (aa409–aa765) Kinasedomänen werden durchgeführt. Die anfängliche In-vitro-Kinase-Inhibitions-Profilierung wird bei einer fixen Konzentration von 1 μM dieser Verbindung durchgeführt. Inhibitorische Konzentration von 50 % (IC50)-Werte werden aus ausgewählten ansprechenden Kinasen, z.B. VEGFR1 und RET, bestimmt. Die TIE2-Kinase-Hemmung wird mit einem homogenen zeitaufgelösten Fluoreszenz (HTRF)-Assay unter Verwendung eines rekombinanten Fusionsproteins von Glutathion-S-Transferase, der intrazellulären Domäne von TIE2 und dem Peptid Biotin-Ahx-EPKDDAYPLYSDFG als Substrat gemessen.
In vivo	Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. This compound prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/21170960/ [2] https://pubmed.ncbi.nlm.nih.gov/21789125/ [3] https://pubmed.ncbi.nlm.nih.gov/22777740/

Anwendungen (Applications)

Methoden	Biomarker	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

Klinische Studieninformationen (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
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

Häufig gestellte Fragen (Frequently Asked Questions)

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

Antwort:
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):

Regorafenib (BAY 73-4506) Multikinase inhibitor

Chemische Struktur

Molekulargewicht: 482.82

Qualitätskontrolle (Quality Control)

Zellkultur, Behandlung & Arbeitskonzentration (Cell Culture, Treatment & Working Concentration)

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Löslichkeit (Solubility)

Molaritätsrechner

In-vivo-Formulierungsrechner (Klare Lösung)

Wirkmechanismus (Mechanism of Action)

Anwendungen (Applications)

Klinische Studieninformationen (Clinical Trial Information)

Häufig gestellte Fragen (Frequently Asked Questions)

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)