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
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.
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. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.