化合物 PND-1186|T1950

價(jià)格	詢價(jià)
包裝	1removed

最小起訂量	1removed
發(fā)貨地	上海
更新日期	2026-05-08

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產(chǎn)品詳情

中文名稱:化合物 PND-1186	英文名稱:PND-1186
CAS:1061353-68-1	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: 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.
純度規(guī)格: 99.61%	產(chǎn)品類別: 抑制劑
貨號(hào): T001\|T1950

Product Introduction

Bioactivity

名稱	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.
細(xì)胞實(shí)驗(yàn)	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)
激酶實(shí)驗(yàn)	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.
體外活性	方法：在多種MPM細(xì)胞（MSTO-211H、H28、Ren、1157等）及非MPM細(xì)胞中，采用AlamarBlue增殖實(shí)驗(yàn)檢測(cè)梯度濃度PND-1186處理72 h后的IC50。結(jié)果：CDH1 mRNA高表達(dá)的MPM細(xì)胞（如Ren、1157）對(duì)PND-1186耐藥（IC50達(dá)7.20–24.86 μM），而低表達(dá)者敏感（IC50 0.70–1.20 μM）；流式細(xì)胞周期分析證實(shí)PND-1186誘導(dǎo)G2/M期阻滯。[1] 方法：在高糖誘導(dǎo)的H9c2及原代心肌細(xì)胞中，采用MTT法確定PND-1186安全劑量（5、10 μM），預(yù)處理1 h后聯(lián)合高糖刺激24–48 h。結(jié)果：PND-1186顯著抑制纖維化（Col-1、TGF-β）、肥大（β-Myhc）及炎癥因子（TNF-α、IL-6、IL-1β）表達(dá)，并阻斷NF-κB活化。[2]
體內(nèi)活性	方法：在STZ誘導(dǎo)的1型糖尿病小鼠模型中，PND-1186以50 mg/kg劑量溶于0.5%羧甲基纖維素鈉緩沖液，每?jī)商炜诜淮?，從糖尿病確診后第9周起連續(xù)治療8周。結(jié)果：PND-1186有效抑制心臟FAK磷酸化，減輕心肌纖維化與肥大，改善射血分?jǐn)?shù)和短軸縮短率，并降低炎癥因子表達(dá)及NF-κB活化。[3]
存儲(chǔ)條件	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.
關(guān)鍵字	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
相關(guān)產(chǎn)品	Urea \| Formamide \| Dimethyl phthalate \| Aceglutamide \| Alginic acid \| Dextran sulfate sodium salt (MW 5000) \| Metronidazole \| Sildenafil citrate \| Citric Acid Triammonium \| Stavudine \| Tamoxifen \| Adenosine
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| NO PAINS 化合物庫(kù) \| 血液病分子庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： VS-4718;SR-2516;PND1186;PND 1186;TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （14年）	注冊(cè)資本	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

TargetMol中國(guó)（陶術(shù)生物）

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公司成立：14年
注冊(cè)資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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