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Regorafenib

Cat. No. M1669
Regorafenib Structure
Synonym:

BAY 73-4506

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM/1mL In DMSO USD 90 In stock
10mg USD 60 In stock
50mg USD 100 In stock
100mg USD 140 In stock
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Quality Control
Biological Activity

Regorafenib (BAY 73-4506) is a novel oral multikinase inhibitor of c-KIT, VEGFR2, B-Raf with IC50s of 17, 40 and 69 nM respectively. Regorafenib (BAY 73-4506) administered once orally at 10 mg/kg significantly decreased the extravasation of Gadomer in the vasculature of rat GS9L glioblastoma tumor xenografts.

Customer Product Validations & Biological Datas
Source Cancer Chemother Pharmacol (2015). Figure 4. Regorafenib
Method MTT assay
Cell Lines HepG2 cells
Concentrations 1 μM
Incubation Time 48 and 72 h
Results We found that the growth inhibition observed with both drugs was significantly higher when they were used in combination (Fig. 4a). In addition, we saw that Erlotinib 1.25 μM also partially blocked the effects of hPLs in antagonizing Regorafenib-mediated cell growth inhibition (Fig. 4b).
Source Cancer Chemother Pharmacol (2015). Figure 1. Regorafenib
Method MTT assay
Cell Lines HCC cell lines
Concentrations 1–5 μM
Incubation Time 48 h
Results As shown in Fig. 1c, after 6 h (T1) from block release, Regorafenib-treated cells in G2/M phase were similar to the control cells at T0, while the number of control cells that proceeded through the cell cycle doubled with respect to the number of cells at T0.
Protocol
Cell Experiment
Cell lines GIST 882, TT cells MDA-MB-231, HepG2 and A375 cells
Preparation method Cell proliferation assays For proliferation assays, GIST 882 and TT cells were grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells were trypsinized, plated at 5 104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37 C. The next day, vehicle or regorafenib serially diluted in complete growth media to between 10µM and 5 nM final concentrations, and 0.2% DMSO, was added and incubation was continued for 96 hr. Cell proliferation was quantified using CellTitre-GloTM (Promega Corporation, Madison, WI).
Concentrations 5nM~10µM
Incubation time 96 h
Animal Experiment
Animal models Mice bearing xenografts of the human CRC cell line Colo-205 (B-RAFV600E), the human BC cell line MDA-MB-231 (K-RASG13D, B-RAFG464V) or the human RCC cell line 786-O (Von-Hippel Lindau gene - /- )
Formulation formulated as a solution in either PEG400/125 mM aqueous methanesulfonic acid (80/20) or polypropylene glycol/PEG400/Pluronic F68 (42.5/42.5/15 þ 20% Aqua)
Dosages 100, 30, 10, and 3 mg/ kg qd 21 in the 786-O model, and qd 9 in the Colo-205 and MDA-MB-231 models
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 482.82
Formula C21H15ClF4N4O3
CAS Number 755037-03-7
Purity 98.71%
Solubility DMSO
Storage at -20°C
References

Regorafenib monotherapy for previously treated metastatic colorectal cancer (CORRECT): an international, multicentre, randomised, placebo-controlled, phase 3 trial.
Grothey A, et al. Lancet. 2013 Jan 26;381(9863):303-12. PMID: 23177514.

Regorafenib (BAY 73-4506) in advanced colorectal cancer: a phase I study.
Strumberg D, et al. Br J Cancer. 2012 May 22;106(11):1722-7. PMID: 22568966.

Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity.
Wilhelm SM, et al. Int J Cancer. 2011 Jul 1;129(1):245-55. PMID: 21170960.

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Keywords: Regorafenib, BAY 73-4506 supplier, VEGFR/PDGFR, inhibitors

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