Apatinib is an orally bioavailable, small-molecule receptor tyrosine kinase inhibitor with potential antiangiogenic and antineoplastic activities. The free-base form is also known as Rivoceranib. Apatinib selectively binds to and inhibits vascular endothelial growth factor receptor 2, which may inhibit VEGF-stimulated endothelial cell migration and proliferation and decrease tumor microvessel density. Apatinib also potently suppresses the activities of Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. Apatinib has no significant effects on EGFR, Her-2 or FGFR1 in concentrations up to 10 μM. Statistically significant growth inhibition is obtained with 50 mg/kg per day Apatinib in three of five tumor xenografts tested. Each tumor xenograft model is significantly growth inhibited by Apatinib at the dose of 100 kg/day. Similar tumor growth inhibition is observed (T/C%, 8% to 18%) in mice following treatment with Apatinib at the dose of 200 kg/day. Full growth inhibition profiles are shown for three of the xenografts.
Appl Biochem Biotechnol Appl Biochem Biotechnol. 2022 Jul 1.
Apatinib Through Activating the RhoA/ROCK Signaling Pathway to Cause Dysfunction of Vascular Smooth Muscle CellsMuscle Cells
Apatinib purchased from AbMole
| Molecular Weight | 397.47 |
| Formula | C24H23N5O |
| CAS Number | 811803-05-1 |
| Solubility (25°C) | DMSO: ≥ 20 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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