Regorafenib (BAY 73-4506) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.
| Molecular Weight | 519.28 |
| Formula | C21H16Cl2F4N4O3 |
| CAS Number | 835621-07-3 |
| Solubility (25°C) | 5.6 mg/mL in 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 |
|---|
| Isolinderalactone
Isolinderalactone suppresses human glioblastoma growth and angiogenic activity through the inhibition of VEGFR2 activation in endothelial cells. Isolinderalactone suppressed the expression of B-cell lymphoma 2 (BCL-2), as well as of survivin and X-linked inhibitor of apoptosis protein (XIAP). |
| Oglufanide
Oglufanide (H-Glu-Trp-OH) is a dipeptide immunomodulator isolated from calf thymus. |
| KLTWQELYQLKYKGI
KLTWQELYQLKYKGI (QK) is a VEGF mimicking peptide, binds to the VEGF receptors and competes with VEGF. |
| 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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