Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PQ401 hydrochloride (196868-63-0(free base)) 抑制 IGF-1R 结构域的自磷酸化,IC50 <1 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 215 | 现货 | ||
2 mg | ¥ 298 | 现货 | ||
5 mg | ¥ 660 | 现货 | ||
10 mg | ¥ 920 | 现货 | ||
25 mg | ¥ 1,630 | 现货 | ||
50 mg | ¥ 2,930 | 现货 | ||
100 mg | ¥ 4,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 685 | 现货 |
产品描述 | PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM. |
靶点活性 | IGF-1R:<1 μM |
体外活性 | PQ 401 is an IGF-1R inhibitor and inhibits autophosphorylation of the IGF-IR kinase domain at concentrations <100 nM, with an IC50 <1 μM. 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. |
体内活性 | PQ 401 (50 mg/Kg, 100 mg/Kg) significantly inhibits MCNeuA tumor growth in a dose-dependent manner. |
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 is then 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). |
细胞实验 | Cell lines: MCF-7,MCNeuA. Concentrations: ~50 μM. Incubation Time: 3 days. Method: 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. |
动物实验 | Animal Models: FVB/N-TgN(MMTVneu)202 mouse injected with MCNeuA cells. Formulation: 8% polysorbate 80 and ethanol. Dosages: 50 or 100 mg/kg. Administration: i.p. |
分子量 | 378.25 |
分子式 | C18H17Cl2N3O2 |
CAS No. | T4324 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (118.97 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6438 mL | 13.2188 mL | 26.4375 mL | 66.0939 mL |
5 mM | 0.5288 mL | 2.6438 mL | 5.2875 mL | 13.2188 mL | |
10 mM | 0.2644 mL | 1.3219 mL | 2.6438 mL | 6.6094 mL | |
20 mM | 0.1322 mL | 0.6609 mL | 1.3219 mL | 3.3047 mL | |
50 mM | 0.0529 mL | 0.2644 mL | 0.5288 mL | 1.3219 mL | |
100 mM | 0.0264 mL | 0.1322 mL | 0.2644 mL | 0.6609 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PQ401 hydrochloride (196868-63-0(free base)) T4324 Tyrosine Kinase/Adaptors IGF-1R PQ-401 hydrochloride (196868-63-0(free base)) PQ401 hydrochloride (196868 63 0(free base)) PQ401 hydrochloride (196868630(free base)) Inhibitor inhibitor inhibit