Tyrphostin AG 879

製品コードS2816 バッチS281601

印刷

化学情報

Chemical Structure Synonyms AG 879 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H24N2OS
分子量 316.46 CAS No. 148741-30-4
Solubility (25°C)* 体外 DMSO 36 mg/mL (113.75 mM)
Ethanol 3 mg/mL (9.47 mM)
Water 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.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.500mg/ml (4.74mM) Taking the 1 mL working solution as an example, add 50 μL of 30 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. 
* <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 Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
in vitro AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. [1] AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. [2] AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. [3] AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937). [4]
in vivo AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. [4] AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells. [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF-7 cells
濃度 20 μM
反応時間 46 hours
実験の流れ

Cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.
動物実験 動物モデル nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
投薬量 20 mg/kg
投与方法 Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15994962/
  • https://pubmed.ncbi.nlm.nih.gov/14726663/
  • https://pubmed.ncbi.nlm.nih.gov/15526167/
  • https://pubmed.ncbi.nlm.nih.gov/16940803/
  • https://pubmed.ncbi.nlm.nih.gov/11419027/
  • https://pubmed.ncbi.nlm.nih.gov/7892601/

カスタマーフィードバック

, , Br J Pharmacol, 2015, 172(13):3370-82.

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：

The molecular and functional landscape of resistance to immune checkpoint blockade in melanoma [ Nat Commun, 2023, 14(1):1516] PubMed: 36934113
The molecular and functional landscape of resistance to immune checkpoint blockade in melanoma [ Nat Commun, 2023, 14(1):1516] PubMed: 36934113
Effect of tyrphostin AG879 on Kv 4.2 and Kv 4.3 potassium channels. [ Br J Pharmacol, 2015, 172(13):3370-82] PubMed: 25752739
Effect of Tyrphostin AG879 on Kv4.2 and Kv4.3 potassium channels 1 Running title: Tyrphostin AG879 inhibits Kv4.2 and Kv4.3 potassium channels [Yu H, et al. Br J Pharmacol, 2015, 10.1111/bph.13127 ]

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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