Sorafenib (BAY 43-9006) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively. Sorafenib induces autophagy and apoptosis. Sorafenib has anti-tumor activity. Sorafenib is also a ferroptosis activator.
Cell Death Dis. 2020 Oct 23;11(10):902.
The miR-30a-5p/CLCF1 axis regulates sorafenib resistance and aerobic glycolysis in hepatocellular carcinoma
Sorafenib (BAY 43-9006) 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
Sorafenib (BAY 43-9006) purchased from AbMole
Phytomedicine. 2015 Dec 1;1139-49.
Polyphyllin I induced-apoptosis is enhanced by inhibition of autophagy in human hepatocellular carcinoma cells.
Sorafenib (BAY 43-9006) purchased from AbMole
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Source | Phytomedicine (2015). Figure 1. Sorafenib was purchased from AbMole (Shanghai, China) |
| Method | Cell viability was determined by MTT assay | |
| Cell Lines | HCC HepG2 | |
| Concentrations | 0~100 µM | |
| Incubation Time | 24, 48, 72 hours | |
| Results | PPI dose- and time-dependently inhibited the proliferation of HepG2 cells, with IC50 values of 1.047 ± 0.376µM within 24 h. Sorafenib was used as a positive control in HepG2 cells. |
| Cell Experiment | |
|---|---|
| Cell lines | PLC/PRF/5, Hep3B, HepG2, HuH7 |
| Preparation method | PLC/PRF/5, Hep3B, HepG2 and HuH7 Cells were seeded in 96-well plates (3,000 cells/well) and incubated overnight for attachment, and were then treated with indicated agents in 10% FBS supplemented medium for 72 hours. The medium was replaced with MTT (0.5 mg/ml) at 37°C for 2 hours. After removal of medium, the cells were lysed with 200 μl per well dimethyl sulfoxide (DMSO), and absorbance at 570 nm was measured and the values of 50% inhibition concentration (IC50) for each drug were determined. |
| Concentrations | 0, 0.25, 0.5,1, 2 µM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | PLC/PRF/5 xenograft model in female athymic nude mice of 4–5 weeks of age |
| Formulation | Dissolved in Cremophor EL/ethanol (50:50; Sigma Cremophor EL, 95% ethanol) at 4 × concentration. |
| Dosages | 60 mg/kg |
| Administration | Po, qd |
| Molecular Weight | 464.82 |
| Formula | C21H16ClF3N4O3 |
| CAS Number | 284461-73-0 |
| Solubility (25°C) | DMSO 45 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.
[3] Xin Chen, et al. Nat Rev Clin Oncol. Broadening horizons: the role of ferroptosis in cancer
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