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Regorafenib

Multi-kinase inhibitor, inhibits VEGFR, PDGFR, FGFR, mutant kit, RET, and Raf-1

Regorafenib

Catalog No. A8236
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
10mg $38.00 In stock
50mg $100.00 In stock
100mg $160.00 In stock
200mg $250.00 In stock

All inclusive: Shipping and all other fees included

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Regorafenib

Related Biological Data

Regorafenib
Regorafenib inhibits growth-factor-stimulated VEGFR2 and VEGFR3 autophosphorylation in human umbilical vascular endothelialcells (HuVECs) and intracellular signaling and migration in lymphatic endothelial cells (LECs). Western blot analysis of (a) VEGFR2 and (b) VEGFR3, ERK1/2 and AKT from total cell lysates from (a) HuVECs and (b) LECs. All cells were treated with the indicated concentrations of regorafenib and subsequently stimulated with (a) VEGF-A or (b) VEGF-C. * indicates nonspecific signals.

Related Biological Data

Regorafenib

Related Biological Data

Regorafenib

Biological Activity

Description Regorafenib (BAY 73-4506) is a multi-target inhibitor of 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, respectively.
Targets VEGFR1/2/3 PDGFRβ Kit RET Raf-1  
IC50 13 nM/4.2 nM/46 nM 22 nM 7 nM 1.5 nM 2.5 nM  

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Chemical Properties

Cas No. 755037-03-7 SDF Download SDF
Synonyms BAY 73-4506
Chemical Name 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide
Canonical 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
Formula C21H15ClF4N4O3.H2O M.Wt 500.83
Solubility Soluble in DMSO Storage Desiccate at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Regorafenib is an orally active multi-kinase inhibitor targeting angiogenic (VEGFR, TIE-2), stromal (PDGFR-β) and oncogenic (RAF, RET and c-KIT) receptor tyrosine kinases, with IC50s of 17, 40 and 69 nM for c-KIT, VEGFR2, B-Raf, respectively.