Axitinib NEW
| Price | $33 | $45 | $61 |
| Package | 25mg | 50mg | 100mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-20 |
Product Details
| Product Name: Axitinib | CAS No.: 319460-85-0 |
| Purity: 99.81% | Supply Ability: 10g |
| Release date: 2024/11/20 |
Product Introduction
Bioactivity
| Name | Axitinib |
| Description | Axitinib (AG-013736) is a multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1, VEGFR2, VEGFR3, and PDGFRβ (IC50=4/20/0.4/2 nM). Axitinib has antitumor activity and is used in the treatment of renal cell carcinoma. |
| Cell Research | Endothelial or tumor cells were starved for 18 h in the presence of either 1% FBS (HUVEC) or 0.1% FBS (tumor cells). Axitinib was added and cells were incubated for 45 min at 37°C in the presence of 1 mmol/L Na3VO4. The appropriate growth factor was added to the cells, and after 5 min, cells were rinsed with cold PBS and lysed in the lysis buffer and a protease inhibitor cocktail. The lysates were incubated with immunoprecipitation antibodies for the intended proteins overnight at 4°C. Antibody complexes were conjugated to protein A beads and supernatants were separated by SDS-PAGE. The Super Signal West Dura kit was used to detect the chemiluminescent signal [1]. |
| Kinase Assay | Porcine aorta endothelial (PAE) cells overexpressing full-length VEGFR-2, PDGFR-β, KIT, and NIH-3T3 overexpressing murine VEGFR-2 (Flk-1) or PDGFR-α were generated as described previously. The ELISA capture plates were prepared by coating 96-well ReactiBind plates with 100 μL/well of 2.5 μg/mL anti-VEGFR-2 antibody, 0.75 μg/mL anti-PDGFR-β antibody, 0.25 μg/mL anti-PDGFR-α antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody. Measurement of RTK phosphorylation by ELISA was done as described previously [1]. |
| Animal Research | AG-013736, a receptor kinase inhibitor of VEGFRs and, at higher doses, PDGFRs (IC50 = 0.1 nmol/L for VEGFR-1, 0.2 nmol/L for VEGFR-2, 0.1–0.3 nmol/L for VEGFR-3, and 1.6 nmol/L for PDGFRβ; ref. 18), was provided by Pfizer Global Research and given once daily by gavage in a volume of 0.13 mL. Control animals received 0.5% carboxymethylcellulose drug carrier. Irradiations were done on nonanesthetized mice using a 137Cs source operating at 2.4 Gy/min. Mice were confined to plastic jigs with tumor-bearing legs extended through an opening in the side, allowing local irradiations. Fractionated doses were given in five daily 2 Gy fractions per week (omitting weekends). For combination treatments, radiotherapy was delivered first, and AG-013736 was given within ～4 h. Mice were sacrificed, and tumors were excised and then quick frozen (using liquid nitrogen) following 1, 2, or 3 weeks of treatment [3]. |
| In vitro | METHODS: Thirteen neuroblastoma cells were treated with Tepotinib for 72 h and cell viability was measured by MTT assay. RESULTS: All cells showed reduced cell viability with IC50 values ranging from 2.4-8.5 μM.[1] METHODS: EBC-1 cells were treated with Tepotinib (0-30 μmol/L) for 3 days, and the expression levels of target proteins were detected by Western Blot. RESULTS: Tepotinib treatment induced a significant reduction in c-Met constitutive phosphorylation in EBC-1 cells with an IC50 of 9 nmol/L. Tepotinib also effectively blocked the phosphorylation of the major downstream effectors of the c-Met enzyme in EBC-1, MKN-45, and Hs746T cells in the 1-10 nmol/L range. [2] |
| In vivo | METHODS: To assay antitumor activity in vivo, Tepotinib (5-15 mg/kg) was injected once daily for 14 days into CD-1 mice bearing EBC-1 xenografts. RESULTS: Administration of 5 or 15 mg/kg of Tepotinib daily to mice bearing EBC-1 tumors effectively inhibited or completely regressed the tumors, respectively. [2] |
| Storage | store at low temperature,keep away from moisture,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 9.7 mg/mL (25 mM) |
| Keywords | inhibit | Platelet-derived growth factor receptor | Inhibitor | Axitinib | Vascular endothelial growth factor receptor | AG013736 | VEGFR | AG 013736 | PDGFR |
| Inhibitors Related | Sorafenib |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Tyrosine Kinase Inhibitor Library | EMA Approved Drug Library | Drug Repurposing Compound Library | Inhibitor Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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