Regorafenib Hydrochloride

SKU: orb1298964

Description

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is an orally bioavailable, small-molecule multikinase inhibitor targeting key angiogenic, stromal, and oncogenic receptor tyrosine kinases. It demonstrates potent antitumor activity in preclinical models, supporting its research use in oncology for both in vitro mechanistic studies and in vivo efficacy experiments.

Research Area

Cardiovascular Research, Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 835621-07-3
• MW: 519.28
• Purity: 99.56% (May vary between batches)
• Formula: C₂₁H₁₆Cl₂F₄N₄O₃
• SMILES: Cl.CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
• Target: c-RET,Raf,VEGFR,PDGFR,Autophagy
• Solubility: DMSO:40 mg/mL (77.03 mM)

Bioactivity

• Target IC50:
  VEGFR1:13 nM|VEGFR3:46 nM|VEGFR2:4.2 nM|B-Raf:28 nM|B-Raf (V600E):19 nM|PDGFRβ:22 nM|Raf-1:2.5 nM
• In Vivo:
  Regorafenib administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts. In a daily (qd)×4 dosing study, the pharmacodynamic effects persisted for 48 hr after the last dosing and correlated with tumor growth inhibition (TGI). A significant reduction in tumor microvessel area was observed in a human colorectal xenograft after qd×5 dosing at 10 and 30 mg/kg. Regorafenib exhibited potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages observed in breast MDA-MB-231 and renal 786-O carcinoma models. Pharmacodynamic analyses of the breast model revealed strong reduction in staining of proliferation marker Ki-67 and phosphorylated extracellular regulated kinases 1/2.
• In Vitro:
  Regorafenib inhibits additional angiogenic kinases (VEGFR1/3, platelet-derived growth factor receptor-β and fibroblast growth factor receptor 1) and the mutant oncogenic kinases KIT, RET and B-RAF.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

cRET, BAY73-4506 Hydrochloride, BAY73-4506 hydrochloride, Autophagy, BAY 73-4506, inhibit, Platelet-derived growth factor receptor, PDGFR, Inhibitor, RET, Regorafenib, Regorafenib Hydrochloride, Raf-1, Raf kinases, Raf, VEGFR, Vascular endothelial growth factor receptor

Compound Identifiers

PubChem CID

66577009