solo per uso di ricerca

Regorafenib (BAY 73-4506) Multikinase inhibitor

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

N. Cat.: 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

Struttura chimica

Peso molecolare: 482.82

Vai a

Controllo Qualità (Quality Control)

Lotto: Purezza: 99.91%

99.91

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

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Formulazione	Descrizione dell'attività	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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	482.82	Formula	C₂₁H₁₅ClF₄N₄O₃	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	755037-03-7	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	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

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 97 mg/mL (200.9 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Ethanol : 3 mg/mL

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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.
Saggio chinasico	Saggi chinasici
Saggio chinasico	Vengono eseguiti saggi in vitro utilizzando i domini chinasi ricombinanti di VEGFR2 (murino aa785–aa1367), VEGFR3 (murino aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) e BRafV600E (aa409–aa765). La profilazione iniziale dell'inibizione chinasica in vitro viene eseguita a una concentrazione fissa di 1 μM di questo composto. I valori di concentrazione inibitoria del 50% (IC50) sono determinati dalle chinasi rispondenti selezionate, ad esempio, VEGFR1 e RET. L'inibizione della chinasi TIE2 viene misurata con un saggio di fluorescenza omogenea risolta nel tempo (HTRF) utilizzando una proteina di fusione ricombinante di glutatione-S-transferasi, il dominio intracellulare di TIE2 e il peptide biotina-Ahx-EPKDDAYPLYSDFG come substrato.
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.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/21170960/ [2] https://pubmed.ncbi.nlm.nih.gov/21789125/ [3] https://pubmed.ncbi.nlm.nih.gov/22777740/

Applicazioni (Applications)

Metodi	Biomarcatori	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

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

Domande Frequenti (Frequently Asked Questions)

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

Risposta:
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):