Toceranib phosphate

製品コードS5272 バッチS527201

印刷

化学情報

Chemical Structure Synonyms Palladia, SU11654 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C22H25FN4O2.H3O4P
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
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <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 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.
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].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BR, C2, and P815 cells
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/12855656/
  • https://pubmed.ncbi.nlm.nih.gov/12091352/

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：

Establishment and characterization of six canine hepatocellular carcinoma cell lines [ Front Vet Sci, 2024, 11:1392728] PubMed: 38840628

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。

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