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Regorafenib (BAY 73-4506)

(CAS No:755037-03-7)
Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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.
CAS No:755037-03-7
Molecular Weight(MW):482.82
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 755037-03-7
Molecular formula(MF) C21H15ClF4N4O3
Molecular Weight(MW): 482.82
Alias BAY 73-4506; 4-[4-({[4-Chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide; BAY 73-4506(Regorafenib); 4-[4-({[4-chioro-3-(trifluoroMethyl)phenyl]carbaMoyl}aMino)-3-fluorophenoxy]-pyridine-2-carboxylic acid MethylaMide; Regorafenib (BAY 73-4506); 4-[4-[[[[4-Chloro-3-(trifluoroMethyl)phenyl]aMino]carbonyl]aMino]-3-fluorophenoxy]-N-Methyl-2-pyridinecarboxaMide; 4-[4-[N'-(4-Chloro-3-trifluoroMethylphenyl)ureido]-3- fluorophenoxy]pyridine-2-carboxylic Acid MethylaMide
Solubility
In vitro DMSO 97 mg/mL (200.9 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
Biological Activity
Description Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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.
Targets
RET [1]
(Cell-free assay)		 Raf-1 [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)		 Kit [1]
(Cell-free assay)		 VEGFR1 [1]
(Cell-free assay)
1.5 nM 2.5 nM 4.2 nM 7 nM 13 nM
In vitro

Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. [1] Regorafenib 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). [2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. [3]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description 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

... Click to View More Cell Line Experimental Data
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. Regorafenib 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. [1]
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