Shopping Cart
- Remove All
![TargetMol](https://www.targetmol.com/storage/error/oops.webp)
Your shopping cart is currently empty
Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $30 | In Stock | |
10 mg | $47 | In Stock | |
25 mg | $73 | In Stock | |
50 mg | $97 | In Stock | |
100 mg | $147 | In Stock | |
500 mg | $369 | In Stock | |
1 mL x 10 mM (in DMSO) | $52 | In Stock |
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, BRAF:28 nM, VEGFR3:46 nM, PDGFRβ:22 nM, Raf-1:2.5 nM, VEGFR2:4.2 nM, B-Raf (V600E):19 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]. |
Alias | BAY73-4506 hydrochloride |
Molecular Weight | 519.28 |
Formula | C21H16Cl2F4N4O3 |
Cas No. | 835621-07-3 |
Storage | |||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (77.03 mM), Sonication is recommended. ![]() | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
|
Copyright © 2015-2024 TargetMol Chemicals Inc. All Rights Reserved.