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Regorafenib Hydrochloride

🥰Excellent
Catalog No. T8402Cas No. 835621-07-3
Alias BAY73-4506 hydrochloride

Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity

Regorafenib Hydrochloride

Regorafenib Hydrochloride

🥰Excellent
Purity: 100%
Catalog No. T8402Alias BAY73-4506 hydrochlorideCas No. 835621-07-3
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
Pack SizePriceAvailabilityQuantity
5 mg$30In Stock
10 mg$47In Stock
25 mg$73In Stock
50 mg$97In Stock
100 mg$147In Stock
500 mg$369In Stock
1 mL x 10 mM (in DMSO)$52In Stock
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Purity:100%
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Product Introduction

Bioactivity
Description
Regorafenib Hydrochloride (BAY73-4506 hydrochloride) is a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity
Targets&IC50
VEGFR1:13 nM, Raf-1:2.5 nM, B-Raf (V600E):19 nM, BRAF:28 nM, PDGFRβ:22 nM, VEGFR3:46 nM, VEGFR2:4.2 nM
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.
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[1].
AliasBAY73-4506 hydrochloride
Chemical Properties
Molecular Weight519.28
FormulaC21H16Cl2F4N4O3
Cas No.835621-07-3
SmilesCl.CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(c3)C(F)(F)F)c(F)c2)ccn1
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (77.03 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9257 mL9.6287 mL19.2574 mL96.2872 mL
5 mM0.3851 mL1.9257 mL3.8515 mL19.2574 mL
10 mM0.1926 mL0.9629 mL1.9257 mL9.6287 mL
20 mM0.0963 mL0.4814 mL0.9629 mL4.8144 mL
50 mM0.0385 mL0.1926 mL0.3851 mL1.9257 mL

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