化合物PQ401 T2085

Product Introduction
Bioactivity


英文名: PQ401

描述: PQ401 (IGF-1R Inhibitor II) 是一种IGF-IR 抑制剂。在 MCF-7 细胞中，它抑制 IGF-I 刺激的 IGF-IR 自磷酸化，可有效抑制 IGF-I 刺激的 MCF-7 细胞生长。它诱导 caspase 介导的细胞凋亡，有用于乳腺癌和其他对 IGF-I 敏感的癌症的研究潜力。

细胞实验: 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.(Only for Reference)

激酶实验: 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), 80 μMEGTA, 0.25% 2-mercaptoethanol, 80 μM Na3VO4, 10 mM MgCl2, and 2 mM MnCl2 for 20 minutes. ATP isthen added at a final concentration of 20 μM. 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).

体内活性: 处理小鼠每周三次通过腹腔注射的方式接受了含有50或100 mg/kg PQ401的溶液，该溶液由8%的聚山梨醇酯80/乙醇/PBS配制而成。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 8.5 mg/mL (25 mM)
DMSO : 17.1 mg/mL (50 mM)


关键字: MCF-7 | IGF-1R | cells | breast | inhibit | caspase | PQ-401 | PQ 401 | PQ401 | Apoptosis | autophosphorylation | cancer | Inhibitor

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相关库: Anti-Aging Compound Library | Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Preclinical Compound Library | Covalent Inhibitor Library

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