[CAS NO. 755037-03-7] Regorafenib (BAY 73-4506)

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PRODUCTS SPECIFICATIONS [755037-03-7]

Catalog

SLK-S1178

Brand

Selleck

CAS

755037-03-7

DESCRIPTION [755037-03-7]

Overview

MDL	MFCD16038047
Molecular Weight	482.82
Molecular Formula	C21H15ClF4N4O3
SMILES	O(C=1C=C(C(NC)=O)N=CC1)C2=CC(F)=C(NC(NC3=CC(C(F)(F)F)=C(Cl)C=C3)=O)C=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.0712 mL	10.3558 mL	20.7117 mL
5 mM	0.4142 mL	2.0712 mL	4.1423 mL
10 mM	0.2071 mL	1.0356 mL	2.0712 mL
50 mM	0.0414 mL	0.2071 mL	0.4142 mL

Description

Regorafenib (BAY 73-4506,Fluoro-Sorafenib, Resihance, Stivarga) 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.

Targets

In vitro

Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppresses 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 KIT and RET, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF-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. 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). Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner.

References

[1] Wilhelm SM, et al. Int J Cancer, 2011, 129(1), 245-255.
[2] Heng DY, et al. Ther Adv Med Oncol, 2010, 2(1), 39-49.
[3] Carr BI, et al. J Cell Physiol, 2013, 228(2), 292-297.

Synonyms

2-Pyridinecarboxamide, 4-[4-[[[[4-chloro-3-(trifluoromethyl)phenyl]amino]carbonyl]amino]-3-fluorophenoxy]-N-methyl-

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

Regorafenib

BAY 73-4506

Stivarga