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Regorafenib Hydrochloride

Regorafenib 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
Catalog No. T8402Cas No. 835621-07-3
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Purity:100%
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Regorafenib Hydrochloride

Catalog No. T8402Cas 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
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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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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, VEGFR2:4.2 nM, VEGFR3:46 nM, BRAF:28 nM, B-Raf (V600E):19 nM, PDGFRβ:22 nM, Raf-1:2.5 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
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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