PND-1186 (VS-4718)

For research use only. Not for use in humans.

目录号:S7653 别名: SR-2156

PND-1186 (VS-4718) Chemical Structure

CAS No. 1061353-68-1

PND-1186 (VS-4718, SR-2156) 是一种可逆的选择性FAK抑制剂,IC50为1.5 nM。PND-1186 可选择性地促进肿瘤细胞的凋亡。Phase 1。

规格 价格 库存 购买数量  
RMB 1199.56 现货
RMB 3867.63 现货
RMB 8164.88 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的PND-1186 (VS-4718)发表文献18篇:

客户使用该产品的5个实验数据:

  • (a) Percentage of apoptotic HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 measured by Annexin V and flow cytometry. Values are plotted as mean±SD (*P<0.05; **P<0.01; versus Vehicle, n =3). (b) Representative WB for p21 and caspase-3 in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (0), 0.5 μM or 1 μM PND 1186. β-tubulin is reported as a loading control (n=2). (c) Relative mRNA expression of EZH2 and NOTCH2 genes as measured by qRT-PCR in HepG2 and Huh7.5 cells after 48 h of treatment with DMSO (Vehicle), 0.5 μM or 1 μM PND 1186 (*P<0.05; **P<0.01; versus Vehicle, n =3).

    Cell Death Differ, 2017, 24(5):889-902. PND-1186 (VS-4718) purchased from Selleck.

  • Cells treated with different concentrations of VS-4718 for 24 h on 3D Matrigel culture were immunostained for cleaved caspase-3 and F-actin (d), and observed using confocal microscopy. Images are representative of cells treated with 10 μM VS-4718. Arrowheads (d) indicate cleaved caspase-3 activity. Data are presented as the means±s.d. of three independent experiments. The bar graphs show the average proportion of PI-positive spheroids. *P<0.01. Scale bar, 50 μm.

    Oncogene, 2017, 36(39):5522-5531. PND-1186 (VS-4718) purchased from Selleck.

  • Cells were added equally to coverslips pretreated with fibronectin at 10 g/ml. Kinase inhibitors were then applied to these cells at the indicated concentrations. U0126 is a MAP kinase inhibitor, PND1186 is an FAK kinase inhibitor, saracatinib is an Src kinase inhibitor, and wortmannin is a PI3K inhibitor. Twenty-five minutes later, cells were pulsed with 2mM5-FUrd for 10 min. Cells were then instantly fixed and stained with anti-BrdU antibody to visualize newly synthesized RNA in situ. Representative images are shown. (First column) 5-FUrd staining. Magnification, ×10. (Third column) 5-FUrd staining. Magnification, ×40. (Second and fourth columns) DAPI staining.

    Molecular and Cellular Biology, 2016, 36(10):1555-1568.. PND-1186 (VS-4718) purchased from Selleck.

  • HIEC cells were treated with FAK inhibitor (1 μM VS-4718), or DMSO for 24 h, then exposed to 5 Gy of radiation and samples were taken 6 and 24 h later. Levels of FAK, p-FAK, and γH2AX were examined using western blotting and GAPDH was used as a loading control.

    Toxicol Appl Pharmacol, 2018, 360:131-140. PND-1186 (VS-4718) purchased from Selleck.

  • Combined treatment of Dasatinib and PND‐1186 results in strong growth inhibition in HCC cell lines. A, Cell viability of HCC3‐4, HCC4‐4, SNU‐398, SNU‐475 cells when treated with Dasatinib, PND‐1186, or Dasatinib+PND‐1186 at ~IC50 concentration determined using crystal violet staining. Data are presented as mean ± SD; and P‐value was calculated using Mann‐Whitney U test. Each dot represents one treatment replicate. B, Expression of p‐Src, Src, p‐FAK and FAK in HCC cell lines analyzed using Western blotting. GAPDH was used as loading control. Das, Dasatinib; Veh, Vehicle

    Cancer Med, 2018, doi:10.1002/cam4.1777. PND-1186 (VS-4718) purchased from Selleck.

产品安全说明书

FAK抑制剂选择性比较

生物活性

产品描述 PND-1186 (VS-4718, SR-2156) 是一种可逆的选择性FAK抑制剂,IC50为1.5 nM。PND-1186 可选择性地促进肿瘤细胞的凋亡。Phase 1。
靶点
FAK [1]
(Cell-free assay)
1.5 nM
体外研究

在体外,PND-1186抑制4T1乳腺癌能动性,在悬浮条件下促进4T1凋亡,并减少4T1软琼脂集落数量和大小。[1]在HEY 和 OVCAR8细胞中,VS-4718促进G0-G1细胞周期阻滞,进而使细胞死亡。[2]

Assay
Methods Test Index PMID
Western blot
pY397 FAK / FAK / pY249 p130Cas / p130Cas / pY416 Src / Src ; 

PubMed: 20234191     


4T1 cells were seeded at 70% confluency on tissue culture plates coated with 10 µg/ml fibronectin. Cells were treated with vehicle (DMSO) or increasing PND-1186 addition for 1 h. Shown is total FAK, p130Cas, Src, or actin levels in cell lysates. Phospho-specific immunoblotting was performed in parallel for changes in FAK or Src activity (pY397 FAK or pY416 Src) and p130Cas tyrosine phosphorylation (pY249 p130Cas). 

β-catenin / Cyclin D1 / c-Myc ; 

PubMed: 25217697     


MM.1S and H929 cells were treated with VS-4718 (0, 2.5, 5, an 10 µM/L) for 24 hours. β-Catenin, c-Myc, and Cyclin D1 expression in these cells was inhibited by VS-4718.

20234191 25217697
Immunofluorescence
STAT3; 

PubMed: 30728047     


Immunofluorescence staining of STAT3 in MDA-MB 231 cells treated for 1 h with 100 nM E2 and 100 nM G1 alone or in combination with 1 μM FAK kinase inhibitor VS-4718. Cells were probed with rabbit anti-STAT3 primary antibody followed by FITC-conjugated secondary antibody in order to detect STAT3 displayed by the green signal, whereas the blue signal indicates the nuclei counterstained with DAPI. Images shown are representative of 10 random fields. 

30728047
Growth inhibition assay
Cell viability ; 

PubMed: 30425643     


Concentration-viability curves for parental and ABCG2- and ABCC1-overexpressing cells incubated with VS-4718. (A) Concentration-viability curves for NCI-H460 and NCI-H460/MX20 cells incubated with VS-4718 for 72 h. (B) Concentration-viability curves for S1 and S1-M1-80 cells incubated with VS-4718 for 72 h. (C)Concentration-viability curves for HEK293/pcDNA3.1 and HEK293/ABCG2 cells incubated with VS-4718 for 72 h. (D) Concentration-viability curves for KB-3-1 and KB-CV60 cells incubated with VS-4718 for 72 h. The cell viability was determined by MTT assay. Data are expressed as mean ±SD, representative of three independent experiments in triplicate.

30425643
体内研究 负荷4T1肿瘤的小鼠体内,PND-1186(100 mg/kg s.c.) 通过诱导细胞凋亡,抑制4T1皮下肿瘤生长。在负荷ID8肿瘤的小鼠体内,PND-1186 (0.5 mg/mL ,p.o.)也会导致卵巢癌肿瘤的生长抑制。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

体外激酶活性试验:

测量GST-FAK在体外的激酶活性,与His标记的FAK 411–686相比,使用K-LISA筛选试剂盒,聚(Glu:Tyr) (4:1)聚合物作为底物固定在微量滴定板上。IC50值用不同浓度的测试化合物在包含50 µM ATP 和 10 mM MnCl2,50 mM HEPES (pH 7.5),25 mM NaCl,0.01% BSA,以及 0.1 mM 原钒酸钠的缓冲液中于室温下测定5分钟。一系列稀释的化合物重复测定3次。底物磷酸化使用辣根过氧化物酶偶联的抗pTyr抗体与光度显色定量。IC50值使用Hill-Slope模型测定。激酶选择性使用激酶分析器进行测定。
细胞实验:[1]
- 合并
  • Cell lines: 小鼠 ID8 卵巢癌细胞
  • Concentrations: ~1 μM
  • Incubation Time: 6天
  • Method: 对于软琼脂测定法,48孔板涂覆1:4混合的2%琼脂(EM Science)和0.2 mL生长培养基(底层)。在0.3%软琼脂的0.2 mL生长培养基(上层)混合物中,每孔接种5×104细胞(重复三份)。琼脂凝固后,加入包含DMSO 或PND-1186 (终浓度0.6 mL)的0.2 mL生长培养基。分解实验中,PND-1186在4天后加入。10天后,菌落被相衬成像,通过计数9个区域(每孔3个区域)进行计算,总面积使用Image J测定。对于所有分析,实验点以一式三份进行,并且至少重复2次。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 负荷ID8肿瘤或4T1肿瘤的小鼠
  • Dosages: 100 mg/kg 每12小时, s.c.;0.5 mg/mL, p.o。
  • Administration: s.c. 或 p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 24 mg/mL (47.85 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 501.5
化学式

C25H26F3N5O3

CAS号 1061353-68-1
储存条件 粉状
溶于溶剂
别名 SR-2156

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01849744 Terminated Drug: VS-4718 Non Hematologic Cancers|Metastatic Cancer Verastem Inc. June 2013 Phase 1
NCT02215629 Withdrawn Drug: VS-4718 Relapsed or Refractory Acute Myeloid Leukemia|Relapsed or Refractory B-Cell Acute Lymphoblastic Leukemia Verastem Inc. Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    Whether the in vivo formulation of PND-1186 (VS-4718) using 2% DMSO+30% PEG 300+5% Tween 80+ddH2O is suitable for injection?

  • 回答:

    The formulation for PND-1186: 2% DMSO+30% PEG 300+5% Tween 80+ddH2O can generate a clear solution with highest contraction at 5mg/ml. It may be suitable for oral administration or injection.

FAK Signaling Pathway Map

相关FAK产品

Tags: 购买PND-1186 (VS-4718) | PND-1186 (VS-4718)供应商 | 采购PND-1186 (VS-4718) | PND-1186 (VS-4718)价格 | PND-1186 (VS-4718)生产 | 订购PND-1186 (VS-4718) | PND-1186 (VS-4718)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID