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PF-9366

PF-9366

产品编号 T5191   CAS 72882-78-1

PF9366 是甲硫氨酸腺苷转移酶 (Mat2A) 抑制剂,其 IC50=420 nM,Kd170 nM。

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PF-9366 Chemical Structure
PF-9366, CAS 72882-78-1
规格 价格/CNY 货期 数量
1 mg ¥ 498 现货
5 mg ¥ 1,236 现货
10 mg ¥ 1,659 现货
25 mg ¥ 2,674 现货
50 mg ¥ 3,996 现货
1 mL * 10 mM (in DMSO) ¥ 1,363 现货
产品目录号及名称: PF-9366 (T5191)
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纯度: 99.74%
纯度: 98.99%
纯度: 97.28%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor (IC50: 420 nM; Kd: 170 nM).
靶点活性 Mat2A:420 nM (cell free)
体外活性 H520 lung carcinoma cells were treated with PF-9366 for 6 h. PF-9366 inhibited cellular SAM production with an IC50 of 1.2 μM. The IC50s of PF-9366 was modestly decreased in the H520 cells with Mat2B knockdown, to 0.86 mM. Huh-7 cells were more sensitive to compound exposure than the H520 cell line. After 6-h exposure to PF-9366, the IC50 for SAM synthesis inhibition was 225 nM.
激酶实验 The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl2, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ?280 of 44,350 /M.cm for Mat2A and an ?280 of 36,440 /M.cm for Mat2B. PF-9366 are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200.
细胞实验 Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with the compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with the compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO2. A 5× solution of cycloleucine is prepared fresh from powder stock in the growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added.
分子量 350.84
分子式 C20H19ClN4
CAS No. 72882-78-1

存储

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

溶解度

DMSO: 20 mg/mL (57 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8503 mL 14.2515 mL 28.503 mL 71.2576 mL
5 mM 0.5701 mL 2.8503 mL 5.7006 mL 14.2515 mL
10 mM 0.285 mL 1.4252 mL 2.8503 mL 7.1258 mL
20 mM 0.1425 mL 0.7126 mL 1.4252 mL 3.5629 mL
50 mM 0.057 mL 0.285 mL 0.5701 mL 1.4252 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Quinlan CL, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792.
AGI-24512 MAT2A-IN-9 AGI-25696 MAT2A inhibitor 4 FIDAS-3 MAT2A-IN-11 AG-270 MAT2A-IN-12

相关化合物库

该产品包含在如下化合物库中:
已知活性化合物库 抑制剂库 NO PAINS 化合物库 表观遗传库 经典已知活性库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

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。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
计算 重置

技术支持

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。

Keywords

PF-9366 72882-78-1 Chromatin/Epigenetic Others Methionine Adenosyltransferase (MAT) inhibit PF 9366 PF9366 Inhibitor inhibitor

 

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