Brivanib (BMS-540215) is an ATP-competitive inhibitor of human VEGFR -2, with an IC50 of 25 nmol/L and Ki of 26 nmol/L. Brivanib is currently in development for the treatment of hepatocellular and colon carcinomas. In vitro and in vivo studies were conducted to characterize the preclinical pharmacokinetics and disposition of brivanib and brivanib alaninate, and antitumor efficacy in mice bearing human xenografts.
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Source | AJR Am J Roentgenol (2014). Figure 3. Brivanib |
| Method | DCE-MRI | |
| Cell Lines | HepG2 cells | |
| Concentrations | 0.01 mL/g | |
| Incubation Time | 14 d | |
| Results | In the brivanib-treated group, the Ktrans and ve values decreased statistically significantly between baseline and 7 days after treatment (p = 0.024 and p = 0.031, respectively), and between baseline and 14 days after treatment (p = 0.043 and p = 0.018), and did not show statistically significant changes between 7 days and 14 days (p = 0.302 and p = 1, respectively). |
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Source | AJR Am J Roentgenol (2014). Figure 2. Brivanib |
| Method | DCE-MRI | |
| Cell Lines | HepG2 cells | |
| Concentrations | 0.01 mL/g | |
| Incubation Time | 14 d | |
| Results | The mean MVD in the tumors that were treated with vehicle and brivanib was approximately 55.2 ± 9.5 vessels/field and 40.8 ± 17.3 vessels/field, respectively (Fig. 2). |
| Cell Experiment | |
|---|---|
| Cell lines | VEGF or FGF stimulated HUVECs |
| Preparation method | The cells are stimulated by VEGF or FGF at a concentration of 8 or 80 ng/mL. These cells are seeded in 96 well plates at a density of 2 × 103 and incubated for 24 hours. Brivanib at various dilutions are added to the cells for another 48 hours. Then 0.5 μCi of [3H] thymidine is added for 24 hours. After that the incorporated tritium is quantified using a β-counter. |
| Concentrations | ~ 10 μM |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | H3396 xenografts in athymic mice |
| Formulation | Dissolved in PEG400: Tween80 (75:25) (orally) or PEG400: water (3:2) (intravenously) |
| Dosages | 60 mg/kg (orally) or 10 mg/kg (intravenously) |
| Administration | oral or i.v. |
| Molecular Weight | 370.38 |
| Formula | C19H19FN4O3 |
| CAS Number | 649735-46-6 |
| Solubility (25°C) | DMSO |
| 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.
| Related VEGFR/PDGFR Products |
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| Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
| KLTWQELYQLKYKGI
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| Protein LMWP
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. |
| CBO-P11
CBO-P11 specifically binds to receptor of VEGFR-2 and is used as targeting ligand for tumor angiogenesis. |
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