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.
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
Axitinib purchased from AbMole
Oncol Res. 2019 Sep 23;27(9):987-995.
Nutlin-3-Induced Sensitization of Non-Small Cell Lung Cancer Stem Cells to Axitinib-Induced Apoptosis Through Repression of Akt1/Wnt Signaling.
Axitinib purchased from AbMole
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
 . figure 6.[1].jpg) |
Source | Int J Cancer (2017) . Figure 6. Axitinib (20 mg/kg, Abmole Bioscience) |
| Method | ||
| Cell Lines | Hmga2/T mice | |
| Concentrations | 20mg/kg | |
| Incubation Time | 6 weeks | |
| Results | Together, these results show that, while bromocriptine and/or axitinib were able to correct structuralabnormalities of tumoral vessels with a similar efficacy, only the combination treatment restored their function. |
 . figure 5..jpg) |
Source | Int J Cancer (2017) . Figure 5. Axitinib (20 mg/kg, Abmole Bioscience) |
| Method | ||
| Cell Lines | Hmga2/T mice | |
| Concentrations | 20mg/kg | |
| Incubation Time | 6 weeks | |
| Results | Analysis of pituitary vasculature in various conditions and morphometric measurements of blood vessels demonstrate that D2R agonist or axitinib had an equivalent capacity to improve structural defects present in tumoral blood vessels and that the combination treatment did not lead to a significant advantage. |
 . figure 4..jpg) |
Source | Int J Cancer (2017) . Figure 4. Axitinib (20 mg/kg, Abmole Bioscience) |
| Method | ||
| Cell Lines | Hmga2/T mice | |
| Concentrations | 20mg/kg | |
| Incubation Time | 6 weeks | |
| Results | Importantly, the expression of Angpt1 and Prok1, which was upregulated in response to bromocriptine treatment, was unchanged and remained low after axitinib treatment (Fig. 4d). |
| Cell Experiment | |
|---|---|
| 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 nM - 10 μM |
| Incubation time | 72 hr |
| Animal Experiment | |
|---|---|
| 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 |
| Molecular Weight | 386.47 |
| Formula | C22H18N4OS |
| CAS Number | 319460-85-0 |
| 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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| AMG-Tie2-1
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