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Synonyms | Palladia, SU11654 | Storage (From the date of receipt) |
3 years -20°C powder | |
化学式 | C22H25FN4O2.H3O4P |
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分子量 | 494.45 | CAS No. | 874819-74-6 | |
Solubility (25°C)* | 体外 | DMSO | 2 mg/mL (4.04 mM) | |
Water | 2 mg/mL (4.04 mM) | |||
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. |
製品説明 | Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. |
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in vitro | Toceranib (SU11654) competes directly with ATP at the intracellular kinase domain of the RTK, thus preventing tyrosine phosphorylation and subsequent signal transduction. In vitro, SU11654 exerts a potent antiproliferative effect on endothelial cells. Additionally, SU11654 treatment can induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in split kinase RTKs[1]. |
in vivo | In mouse xenograft models, oral administration of SU11654 and related compounds affects the growth of multiple tumor cell lines originating from a variety of tissues, leading to either tumor regression or tumor growth inhibition[1]. |
細胞アッセイ | 細胞株 | BR, C2, and P815 cells |
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濃度 | 0.01 to 1 μM | |
反応時間 | 24, 48, and 72 hours | |
実験の流れ | The BR, C2, and P815 cells were counted and resuspended in 24-well plates at a concentration of 0.5 × 106 cells/well (BR and C2) or 0.25 × 106 cells/well (P815) in complete medium. Cells were left untreated, or SU11652, SU11654, or SU11655 was added to a final concentration of 0.01 to 1 μM. Cells were collected after 24, 48, and 72 hours of culture and were counted to determine the number of cells surviving. |
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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。