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.
Cell Death Dis. 2020 Oct 23;11(10):902.
The miR-30a-5p/CLCF1 axis regulates sorafenib resistance and aerobic glycolysis in hepatocellular carcinoma
Regorafenib purchased from AbMole
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Regorafenib purchased from AbMole
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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). |
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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. |
| 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 |
| Molecular Weight | 482.82 |
| Formula | C21H15ClF4N4O3 |
| CAS Number | 755037-03-7 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
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