Axitinib blocked phosphorylation of VEGFR-2 and VEGFR-3 with average IC50s of 0.2 and 0.1 to 0.3 nM.Axitinib (also known as AG013736) is a small molecule tyrosine kinase inhibitor.It inhibits multiple targets, including VEGFR-1, VEGFR-2, VEGFR-3, platelet derived growth factor receptor (PDGFR), and cKIT (CD117). It has been shown to significantly inhibit growth of breast cancer in xenograft models and has been successful in trials with renal cell carcinoma (RCC) and several other tumor types.
Int J Cancer. 2017 May 1;140(9):2150-2161.
Complementary actions of dopamine D2 receptor agonist and anti-vegf therapy on tumoral vessel normalization in a transgenic mouse model
Axitinib purchased from AbMole
Cell Experiment | |
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Cell lines | HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines |
Preparation method | MTS cell proliferation assay HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cell lines were seeded at 5,000 cells per well in a 96-well plate and left to settle overnight in EMBV R-2 or DMEM with 10% fetal calf serum. The cells were treated with axitinib at concentrations ranging from 1 nmol/l to 10 lmol/l. Cell viability was determined after 72 hr using MTS tetrazolium substrate (CellTiter 96 Aqueous One Solution Cell Proliferation Assay; Promega Corporation, Charbonnieres, France) and colorimetric measurement at 490 nm in an automatic plate reader (Elx808; Fisher Bioblock Scientific SAS, Illkirch, France). IC50 values were calculated using GraphPadV R Prism software (version 3.00). |
Concentrations | 1 nmol/l to 10 lmol/l |
Incubation time | 72 hr |
Animal Experiment | |
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Animal models | IGR-N91 xenografts with female SPF-Swiss athymic nude mice at 6–8 weeks of age |
Formulation | 0.5% CMC |
Dosages | 30 mg/kg BID for 2 weeks |
Administration | oral gavage |
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
Molecular Weight | 386.47 |
Formula | C22H18N4OS |
CAS Number | 319460-85-0 |
Purity | 99.80% |
Solubility | DMSO |
Storage | at -20°C |
Comprehensive overview of axitinib development in solid malignancies: focus on metastatic renal cell carcinoma.
Carmichael et al. Clin Adv Hematol Oncol. 2012 May;10(5):307-14. PMID: 22706540.
Evaluation of the effect of food on the pharmacokinetics of axitinib in healthy volunteers.
Pithavala et al. Cancer Chemother Pharmacol. 2012 Jul;70(1):103-12. PMID: 22644797.
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