PQ 401

製品コードS8003 バッチS800301

印刷

化学情報

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

C18H16ClN3O2
分子量 341.79 CAS No. 196868-63-0
Solubility (25°C)* 体外 DMSO 32 mg/mL (93.62 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
30%PEG400 0.5%Tween80 5%propylene glycol
5.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 16.67 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O Dilute 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 PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
in vitro PQ 401 is an IGF-1R inhibitor and inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1μM. PQ 401 significantly reduced proliferation of MCF-7 cells with IC50 of 8 μM. PQ 401 also inhibits growth of MCNeuA cells with IC50 of 15 μM. PQ 401 inhibits the IGF-I-mediated antiapoptotic pathway in MCF-7 cells. PQ 401 increases caspase-mediated apoptotic activity in MCF-7 cells. [1]
in vivo PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner. [1]

プロトコル(参考用のみ)

キナーゼアッセイ IGF-IR Peptide Autophosphorylation
One microgram of constitutively active IGF-IR kinase domain peptide isincubated +/− varying concentrations of PQ 401 in 2% DMSO in 40 mM Tris (pH 7.4), 80μMEGTA, 0.25% 2-mercaptoethanol, 80μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20μM. Autophosphorylation of the kinase domain peptide isallowed to occur for 20 minutes at 22℃. The reaction isstopped by the addition of SDS-reducing buffer and the samples are run on SDS-PAGE. Following transfer to nitrocellulose membrane, peptide autophosphorylation isdetermined by Western blotting employing an antibody against phosphotyrosine (PY20).
細胞アッセイ 細胞株 MCF-7, MCNeuA
濃度 ~50 μM
反応時間 3 days
実験の流れ The inhibitory effects of diaryl urea on breast cancer cell growth are determined using a CyQuant cell proliferation assay kit. MCF-7 or MCNeuA cells are plated in 96-well plates (5 × 103 per well) in phenol red-free DMEM supplemented with 10% FCS. One plate isprepared for each harvest day. Cells are allowed to adhere overnight and are then treated with various concentrations of diaryl urea or DMSO as a vehicle control. Microplate cultures are harvested on days 0, 1, 2, and 3 by inverting the microplate onto paper towels with gentle blotting to remove growth medium without disrupting adherent cells. Each plate iskept at −80 ℃ until the end of the experiment (day 3) when all of the plates are thawed and assayed together. After thawing, 200 μL of CyQuant GR solution are added to each well and the plates are incubated in the dark for 2 to 5 minutes. Fluorescence ismeasured with a SpectraMax Gemini XS fluorescence microplate reader with 480-nm excitation and 520-nm emission. Proliferation index iscalculated as the percent of nucleotide content versus control cells at day 0.
動物実験 動物モデル FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells.
投薬量 50 or 100 mg/kg
投与方法 i.p.

カスタマーフィードバック

Data from [Data independently produced by , , Lung Cancer, 2015, 90(2):175-81]

Data from [Data independently produced by , , Acta Pharmacol Sin, 2018, 39(12):1894-1901]

Data from [Data independently produced by , , J Chemother, 2016, 28(1):44-9.]

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：

MNK1 inhibitor CGP57380 overcomes mTOR inhibitor-induced activation of eIF4E: the mechanism of synergic killing of human T-ALL cells [Huang XB, et al. Acta Pharmacol Sin, 2018, 39(12):1894-1901] PubMed: 30297804
PQ401, an IGF-1R inhibitor, induces apoptosis and inhibits growth, proliferation and migration of glioma cells [Zhou X, et al. J Chemother, 2016, 28(1):44-9] PubMed: 25971682
Reduced expression of EI24 confers resistance to gefitinib through IGF-1R signaling in PC9 NSCLC cells [Choi JM, et al. Lung Cancer, 2015, 90(2):175-81] PubMed: 26342551

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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