Axitinib

製品コードS1005 バッチS100501

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 35 mg/mL warmed with 50ºC water bath (90.56 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

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Piezo1 regulates meningeal lymphatic vessel drainage and alleviates excessive CSF accumulation [ Nat Neurosci, 2024, 10.1038/s41593-024-01604-8] PubMed: 38528202
Targeting PDGF signaling of cancer-associated fibroblasts blocks feedback activation of HIF-1α and tumor progression of clear cell ovarian cancer [ Cell Rep Med, 2024, S2666-3791(24)00201-5] PubMed: 38670097
FLT1 activation in cancer cells promotes PARP-inhibitor resistance in breast cancer [ EMBO Mol Med, 2024, 10.1038/s44321-024-00094-2] PubMed: 38956205
The molecular basis of Abelson kinase regulation by its αI-helix [ Elife, 2024, 12RP92324] PubMed: 38588001
ROCK and the actomyosin network control biomineral growth and morphology during sea urchin skeletogenesis [ Elife, 2024, 12RP89080] PubMed: 38573316
Transcription of microRNAs is regulated by developmental signaling pathways and transcription factors [ Front Cell Dev Biol, 2024, 12:1356589] PubMed: 38721525
New Anti-Angiogenic Therapy for Glioblastoma With the Anti-Depressant Sertraline [ Cancer Med, 2024, 13(20):e70288] PubMed: 39440923
Cardiomyocyte crosstalk with endothelium modulates cardiac structure, function, and ischemia-reperfusion injury susceptibility through erythropoietin [ Front Physiol, 2024, 15:1397049] PubMed: 39011088
Xuebijing improves intestinal microcirculation dysfunction in septic rats by regulating the VEGF-A/PI3K/Akt signaling pathway [ World J Emerg Med, 2024, 15(3):206-213] PubMed: 38855370
Expression and Transcriptional Targets of TGFβ-RII in Paracentrotus lividus Larval Skeletogenesis [ Genesis, 2024, 62(4):e23614] PubMed: 39139086

長期の保管のために-20°Cの下で製品を保ってください。

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。