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PP2

PP2

产品编号 T6266   CAS 172889-27-9
别名: AGL 1879, AG 1879,AGL 1879

PP2 (AG 1879,AGL 1879) 是 Lck/Fyn 抑制剂 (IC50:4/5 nM),对 EGFR 的效力降低约 100 倍,对 ZAP-70、PKA 和 JAK2 无活性。

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PP2 Chemical Structure
PP2, CAS 172889-27-9
规格 价格/CNY 货期 数量
2 mg ¥ 313 现货
5 mg ¥ 489 现货
10 mg ¥ 852 现货
25 mg ¥ 1,420 现货
50 mg ¥ 2,080 现货
100 mg ¥ 3,480 现货
200 mg ¥ 4,890 现货
1 mL * 10 mM (in DMSO) ¥ 547 现货
产品目录号及名称: PP2 (T6266)
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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 PP2 (AG 1879,AGL 1879) is a effective inhibitor of Lck/Fyn (IC50:4/5 nM) , ~100-fold less potent to EGFR, inactive for ZAP-70, PKA and JAK2.
靶点活性 Fyn:5 nM, Lck:4 nM
体外活性 在局灶性脑缺血损伤的大鼠中,PP2()降低约50%梗死面积.在局灶性脑缺血损伤的大鼠中,与对照组相比,PP2(1.5 mg/kg,i.p.)具有更好的神经功能评分.在脾脏接种HT29细胞的SCID小鼠中,与对照组相比,PP2(5 mg/kg/day)降低原代肿瘤的生长率,且明显降低相对肝重和肝转移量.
体内活性 1-100 mM PP2剂量依赖性抑制人类结肠癌细胞(SW480,HT29和PMCO1),肝癌细胞(KYN-2,Li7,PLC/PRF/5和HepG2)和乳腺癌细胞(MDA-MB-468,MCF-7,和 BT-474)生长。在NIH3T3 和NIH-RET/PTC3 细胞裂解液中,5 μM PP2可抑制体内RET/PTC1肿瘤蛋白的磷酸化和信号。在转化RET/PTC1的NIH3T3成纤维细胞、携带自发性RET/PTC1重排的两种人类甲状腺乳头状癌细胞系TPC1 和 FB2中,5 μM PP2抑制血清非依赖性的生长。5 μM PP2抑制TPC1细胞I型胶原基质入侵。在HeLa 和 SiHa 细胞中,10 μM PP2下调pSrc-Y416,pEGFR-Y845和-Y1173 表达水平。10 μM PP2可以调节细胞周期停滞,这是通过上调HeLa和SiHa细胞的p21(Cip1) 和 p27(Kip1),及下调HeLa细胞的cyclin A和细胞周期蛋白依赖性激酶-2,-4 (Cdk-2,-4)的表达,和下调SiHa细胞的cyclin B 和 Cdk-2表达实现的。20 μM PP2抑制40-50% HT29 细胞生长,处理1小时,该浓度降低Src活性,并维持抑制35%Src活性达2天。20 μM PP2明显促进大部分癌细胞(HT29, SW480, PMCO1, PLC/PRF/5, KYN-2, Li7, MCF-7和 MDA-MB-468)聚合,该作用有E-钙粘蛋白依赖性。在癌细胞中,20 μM PP2增强E-钙粘蛋白表达,且强促进E-钙粘蛋白与肌动蛋白细胞骨架的关联。在HT29细胞中,20 μM PP2增强α-catenin,β-catenin和 γ-catenin表达,而在PLC/PRF/5 和 MCF-7细胞,α-catenin的总蛋白水平没有改变,但β-catenin 和 γ-catenin水平稍微增长。
激酶实验 Immune complex enzyme assays: The acid-treated enolase is diluted 1:20 with 1&times PBS before aliquoting 100 mL/well into a Nunc 96-well high protein binding assay plate. Assay wells are then aspirated; blocked with 0.5% bovine serum, 1&times PBS for 1 h at 37 ℃;and then washed five times with 300 mL of 1&times PBS/well. The source of Lck is either LSTRA cells or Lck expressed in HeLa cells using a vaccinia expression system. FynT is expressed in HeLa cells using the vaccinia system. Cells (12.5&times 106/mL) are lysed in lysis buffer (20 mM Tris, pH 8.0, 150 mM NaCl, 0.5% Nonidet P-40, and 23 trypsin inhibitory units/mL aprotinin), and the lysates are clarified by centrifugation at 14,000 cpm for 15 min at 4 ℃ in an Eppendorf tube. The clarified lysates are then incubated with the appropriate anti-kinase antibody at 10 μg/mL for 2 h at 4 ℃. Protein A-Sepharose beads are added to the antibody/lysate mixture at 250 μL/mL and allowed to incubate for 30 min at 4 ℃. The beads are then washed twice in 1 mL of lysis buffer and twice in 1 mL of kinase buffer (25 mM HEPES, 3 mM MnCl2, 5 mM MgCl2, and 100 μM sodium orthovanadate) and resuspended to 50% (w/v) in kinase buffer. Twenty-five microliters of the bead suspension is added to each well of the enolase-coated 96-well high protein binding plate together with an appropriate concentration of compound and [γ-32P]ATP (25 μL/well of a 200 μCi/mL solution in kinase buffer). After incubation for 20 min at 20 ℃, 60 μLl of boiling 2&times solubilization buffer containing 10 mM ATP is added to the assay wells to terminate the reactions. Thirty microliters of the samples is removed from the wells, boiled for 5 min, and run on a 7.5% SDS-polyacrylamide gel. The gels are subsequently dried and exposed to Kodak X-AR film. For quantitation, films are scanned using a Molecular Dynamics laser scanner, and the optical density of the major substrate band, enolase p46, is determined.In companion experiments for measuring the activity of compounds against Lck, the assay plate is washed with two wash cycles on a Skatron harvester using 50 mM EDTA, 1 mM ATP. Scintillation fluid (100 μL) is then added to the wells, and 32P incorporation is measured using a micro-β-counter.
细胞实验 Cell viability is determined using an in vitro toxicology assay kit following the manufacturer's instructions. Cells are seeded in 96-well plates at day 0. Starting at day 1, cells are treated for 2 days with each of a series of increasing concentrations of PP2 (1 μM, 10 μM, and 100 μM). At the end of this period, cell proliferation is evaluated by a colorimetric assay based on the cleavage of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide by mitochondria dehydrogenase in viable cells, leading to formazan formation. This experiment is repeated three times with 10 determinations/tested concentration.(Only for Reference)
别名 AGL 1879, AG 1879,AGL 1879
分子量 301.77
分子式 C15H16ClN5
CAS No. 172889-27-9

存储

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

溶解度

DMSO: 56 mg/mL (185.6 mM)

Ethanol: 2 mg/mL (6.62 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 / Ethanol 1 mM 3.3138 mL 16.5689 mL 33.1378 mL 82.8446 mL
5 mM 0.6628 mL 3.3138 mL 6.6276 mL 16.5689 mL
DMSO 10 mM 0.3314 mL 1.6569 mL 3.3138 mL 8.2845 mL
20 mM 0.1657 mL 0.8284 mL 1.6569 mL 4.1422 mL
50 mM 0.0663 mL 0.3314 mL 0.6628 mL 1.6569 mL
100 mM 0.0331 mL 0.1657 mL 0.3314 mL 0.8284 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. Hanke JH, et al. J Biol Chem, 1996, 271(2), 695-701. 2. Karni R, et al. FEBS Lett, 2003, 537(1-3), 47-52. 3. Nam JS, et al. Clin Cancer Res, 2002, 8(7), 2430-2436. 4. Kong L, et al. Mol Cell Biochem, 2011, 348(1-2), 11-19. 5. Lennmyr F, et al. Acta Neurol Scand, 2004, 110(3), 175-179. 6. Inoue A, et al. Phosphorylation of NMDA receptor GluN2B subunit at Tyr1472 is important for trigeminal processing of itch. Eur J Neurosci. 2016 Oct;44(7):2474-2482.

文献引用

1. Zheng T, Wang H Y, Chen Y, et al. Src Activation Aggravates Podocyte Injury in Diabetic Nephropathy via Suppression of FUNDC1-Mediated Mitophagy. Frontiers in Pharmacology. 2022, 13: 897046-897046 2. Liu K, Hao Z, Zheng H, et al.Repurposing of rilpivirine for preventing platelet β3 integrin-dependent thrombosis by targeting c-Src active autophosphorylation.Thrombosis Research.2023
Tyk2-IN-3 Ginsenoside Ra1 Deucravacitinib SAR-20347 JAK-IN-21 NVP-BSK805 2HCl (1092499-93-8(free base)) Ruxolitinib (S enantiomer) RO495

相关化合物库

该产品包含在如下化合物库中:
高选择性抑制剂库 酪氨酸激酶分子库 抗结直肠癌化合物库 免疫/炎症分子化合物库 细胞重编程化合物库 表观遗传库 抗乳腺癌化合物库 抗卵巢癌化合物库 抗肝癌化合物库 抗衰老化合物库

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

PP2 172889-27-9 Angiogenesis Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Src JAK Tyrosine Kinases EGFR AGL 1879 AG 1879,AGL-1879 AG 1879,AGL 1879 AGL-1879 Inhibitor AGL1879 inhibit PP-2 AG 1879,AGL1879 PP 2 inhibitor

 

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