Alofanib (RPT835)

製品コードS8754 バッチS875401

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C19H15N3O6S
分子量 413.40 CAS No. 1612888-66-0
Solubility (25°C)* 体外 DMSO 83 mg/mL (200.77 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO Corn oil
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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 Alofanib (RPT835) is a novel selective allosteric inhibitor of FGFR2 and has a dramatic inhibitory effect with IC50 <10 nM on FGF2-induced phoshphorylation of FRS2a in KATO III cells. It has no direct effect on FGF2-dependent FGFR1 and FGFR3 phosphorylation levels in either cell lines and no effects on FGF2-FGFR2 binding.
in vitro

Alofanib induces mainly apoptosis with cleavage of caspase 3, PARP and Bcl-2 in SKOV3 cell line. Cytotoxic effect of compound on ovarian cancer cells is low[1]. Alofanib inhibits phosphorylation of FRS2α with the IC50 values of 7 and 9 nmol/l in cancer cells expressing different FGFR2 isoforms. In a panel of four cell lines representing several tumour types (triple-negative breast cancer,melanoma, and ovarian cancer), alofanib inhibits FGF-mediated proliferation with 50% growth inhibition (GI50) values of 16-370 nmol/l. Alofanib dose dependently inhibits the proliferation and migration of human and mouse endothelial cells (GI50: 11-58 nmol/l) compared with brivanib and bevacizumab[2].
in vivo

Intravenous alofanib significantly in dose-dependent manner potentiated the efficiency of the combination of paclitaxel and carboplatin. Alofanib suppresses angiogenesis in ovarian cancer mouse model[1]. In a FGFR-driven human tumour xenograft model, oral administration of alofanib is well tolerated and results in potent antitumour activity[2].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SKOV3 cells
濃度 0-1 μM
反応時間 72 h
実験の流れ

Cells were treated with alofanib (10, 100, and 1000 μM) for 72 h and whole-cell lysates were immunoblotted.
動物実験 動物モデル C57Bl/6 × DBA/2 F1 mice
投薬量 15 mg/kg/d
投与方法 i.p.

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：

Lenvatinib for effectively treating antiangiogenic drug-resistant nasopharyngeal carcinoma [ Cell Death Dis, 2022, 13(8):724] PubMed: 35985991
FGF-2 signaling in nasopharyngeal carcinoma modulates pericyte-macrophage crosstalk and metastasis [ JCI Insight, 2022, e157874] PubMed: 35439170

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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