化合物 PND-1186|T1950

PND-1186
1061353-68-1

询价 1removed 起订

上海更新日期：2026-05-08

TargetMol中国（陶术生物）

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联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 PND-1186

英文名称：: PND-1186

CAS号：: 1061353-68-1

品牌：: TargetMol

产地：: 美国

保存条件：: Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

纯度规格：: 99.61%

产品类别：: 抑制剂

货号：: T001|T1950

Product Introduction

Bioactivity

名称	PND-1186
描述	PND-1186 (VS-4718) is a small molecule inhibitor, a highly specific, reversible FAK inhibitor (IC50=1.5 nM) with good selectivity and cell permeability. This compound inhibits FAK phosphorylation, blocking tumor cell survival, proliferation, migration, and angiogenesis, and is primarily used for anti-tumor research on solid tumors.
细胞实验	For soft agar assays, 48-well plates are coated with a 1:4 mix of 2% agar (EM Science) in 0.2 mL growth media (bottom layer). 5×104 cells are plated per well (in triplicate) in a mixture of 0.3% agar in 0.2 mL growth media (top layer). After agar solidification, 0.2 mL growth media is added containing DMSO or PND-1186 (final concentration for 0.6 mL). In separate experiments, PND-1186 is added after 4 days. After 10 days, colonies are imaged in phase contrast, enumerated by counting 9 fields (3 fields per well), and total area determined using Image J. For all analyses, experimental points are performed in triplicate and repeated at least two times. (Only for Reference)
激酶实验	In vitro kinase activity: GST-FAK in vitro kinase activity is measured and compared to His-tagged FAK 411–686 using the K-LISA screening kit and poly(Glu:Tyr) (4:1) copolymer as a substrate immobilized on microtiter plates. IC50 values are determined with various concentrations of test compounds in a buffer containing 50 μM ATP and 10 mM MnCl2, 50 mM HEPES (pH 7.5), 25 mM NaCl, 0.01% BSA, and 0.1 mM Na orthovanadate for 5 min at room temperature. Serial diluted compounds are tested in triplicate. Substrate phosphorylation is measured using horseradish peroxidase-conjugated anti-pTyr antibodies with spetrophotometric color quantitation. IC50 values are determined using the Hill-Slope Model. Kinase selectivity profiling is performed by using the KinaseProfiler service.
体外活性	方法：在多种MPM细胞（MSTO-211H、H28、Ren、1157等）及非MPM细胞中，采用AlamarBlue增殖实验检测梯度浓度PND-1186处理72 h后的IC50。结果：CDH1 mRNA高表达的MPM细胞（如Ren、1157）对PND-1186耐药（IC50达7.20–24.86 μM），而低表达者敏感（IC50 0.70–1.20 μM）；流式细胞周期分析证实PND-1186诱导G2/M期阻滞。[1] 方法：在高糖诱导的H9c2及原代心肌细胞中，采用MTT法确定PND-1186安全剂量（5、10 μM），预处理1 h后联合高糖刺激24–48 h。结果：PND-1186显著抑制纤维化（Col-1、TGF-β）、肥大（β-Myhc）及炎症因子（TNF-α、IL-6、IL-1β）表达，并阻断NF-κB活化。[2]
体内活性	方法：在STZ诱导的1型糖尿病小鼠模型中，PND-1186以50 mg/kg剂量溶于0.5%羧甲基纤维素钠缓冲液，每两天口服一次，从糖尿病确诊后第9周起连续治疗8周。结果：PND-1186有效抑制心脏FAK磷酸化，减轻心肌纤维化与肥大，改善射血分数和短轴缩短率，并降低炎症因子表达及NF-κB活化。[3]
存储条件	Store at low temperature Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度	10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.99 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 34 mg/mL (67.8 mM), Sonication is recommended.
关键字	VS4718 \| VS 4718 \| tumor \| survival \| SR2516 \| SR 2516 \| PTK2 protein tyrosine kinase 2 \| PTK2 \| PND-1186 \| integrin \| Inhibitor \| inhibit \| growth \| Focal adhesion kinase \| FAK \| cell \| Apoptosis
相关产品	Formamide \| Urea \| Sodium Molybdate \| Dimethyl phthalate \| Aceglutamide \| Alginic acid \| Cysteamine hydrochloride \| Metronidazole \| Sildenafil citrate \| Citric Acid Triammonium \| Stavudine \| Tamoxifen
相关库	抑制剂库 \| 抗癌活性化合物库 \| 经典已知活性库 \| 抗癌化合物库 \| 已知活性化合物库 \| ReFRAME 相关化合物库 \| 激酶抑制剂库 \| 膜蛋白靶向化合物库 \| 药物功能重定位化合物库 \| 酪氨酸激酶分子库 \| 抗癌临床化合物库 \| 抗癌药物库

VS-4718;SR-2516;PND1186;PND 1186;TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(14年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子