Axitinib

製品コードS1005 バッチS100515

印刷

化学情報

Chemical Structure Synonyms AG 013736 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H18N4OS
分子量 386.47 CAS No. 319460-85-0
Solubility (25°C)* 体外 DMSO 40 mg/mL warmed with 50ºC water bath (103.5 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.
in vitro Axitinib could block the cellular autophosphorylation of VEGFR and VEGF-mediated endothelial cell viability, tube formation, and downstream signaling. Axitinib inhibits the proliferation of variable cell lines with IC50 of >10,000 nM (IGR-N91), 849 nM (IGR-NB8), 274 nM (SH-SY5Y) and 573 nM (non-VEGF stimulated HUVEC). [2]
in vivo Axitinib exhibits primary inhibition to orthotopically transplanted models such as M24met (melanoma), HCT-116 (colorectal cancer), and SN12C (renal cell carcinoma). [1] Axitinib delays the tumor growth with 11.4 days compared to the controls (p.o. 30 mg/kg) and decreases the Mean Vessels Density (MVD) to 21, compared to 49 in controls, in IGR-N91 flank xenografts. [2] Axitinib significantly inhibits growth and disrupts tumor microvasculature in BT474 breast cancer model at 10-100 mg/kg. [3] Axitinib has shown single-agent activity in variable tumors, including renal cell carcinoma, thyroid cancer, non-small cell lung cancer, and melanoma.
特徴 Superior as second-line therapy relative to sorafenib (current standard-of-care).

プロトコル(参考用のみ)

キナーゼアッセイ Cellular receptor kinase phosphorylation assay
Porcine aorta endothelial (PAE) cells, which overexpress full-length VEGFR2, PDGFRβ, Kit, and NIH-3T3, which overexpress murine VEGFR2 (Flk-1) or PDGFRα, are generated. The 96-well plates are coated with 100 μL/well of 2.5 μg/mL anti-VEGFR2 antibody, 0.75 μg/mL anti-PDGFRβ antibody, 0.25 μg/mL anti-PDGFRα antibody, 0.5 μg/mL anti-KIT antibody, or 1.20 μg/mL anti-Flk-1 antibody to prepare ELISA capture plates. Then phosphorylation of RTK is measured by ELISA.
細胞アッセイ 細胞株 HUVEC, SH-SY5Y, IGR-N91 and IGR-NB8 cells
濃度 1 nM - 10 μM
反応時間 72 hours
実験の流れ

Cells are seeded in a 96-well plate at a density of 5 × 104 and cultured for 24 hours. Axitinib is added to the cells at concentrations ranging from 1 nM to 10 μM. Cell viability is measured after 72 hours by MTS tetrazolium substrate and IC50 values are calculated.
動物実験 動物モデル BT474 breast cancer cells are implanted subcutaneously into Immune-deficient female mice (Nu/nu; age 8-12 weeks).
投薬量 10, 30 or 100 mg/kg
投与方法 Oral daily

カスタマーフィードバック

Data from [J Biomol Screen, 2011, 16, 141-154]

, , Oncogene, 2017, 36(36):5098-5109

, , Dr. Cheri Pasch of UW Madison

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人間や獣医の診断であるか治療的な使用のためにでない。

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