Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PND-1186 (VS-4718) 是一种高特异性的FAK 可逆抑制剂,IC50为 1.5 nM。它选择性促进肿瘤细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 221 | 现货 | ||
5 mg | ¥ 492 | 现货 | ||
10 mg | ¥ 759 | 现货 | ||
25 mg | ¥ 1,520 | 现货 | ||
50 mg | ¥ 2,280 | 现货 | ||
100 mg | ¥ 3,420 | 待询 |
产品描述 | PND-1186 (VS-4718) is a reversible and specific FAK inhibitor (IC50: 1.5 nM). |
靶点活性 | FAK:1.5 nM |
体外活性 | 在负荷4T1肿瘤的小鼠体内,PND-1186(100 mg/kg,s.c.)可诱导细胞凋亡,对4T1皮下肿瘤生长产生抑制作用.在负荷ID8肿瘤的小鼠体内,PND-1186(0.5 mg/mL,p.o.)还会抑制卵巢癌肿瘤的生长. |
体内活性 | 在体外,PND-1186对4T1乳腺癌能动性有抑制作用,且可促进悬浮状态的4T1凋亡,并使4T1软琼脂集落数量和大小减少。在HEY 和 OVCAR8细胞中,PND-1186促使G0-G1细胞周期阻滞,从而使细胞死亡。 |
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. |
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) |
别名 | PND1186, PND 1186, VS-4718, SR-2516 |
分子量 | 501.5 |
分子式 | C25H26F3N5O3 |
CAS No. | 1061353-68-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 23 mg/mL (45.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.994 mL | 9.9701 mL | 19.9402 mL | 49.8504 mL |
5 mM | 0.3988 mL | 1.994 mL | 3.988 mL | 9.9701 mL | |
10 mM | 0.1994 mL | 0.997 mL | 1.994 mL | 4.985 mL | |
20 mM | 0.0997 mL | 0.4985 mL | 0.997 mL | 2.4925 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
PND-1186 1061353-68-1 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK tumor integrin PTK2 inhibit growth Focal adhesion kinase PND1186 PTK2 protein tyrosine kinase 2 PND 1186 VS-4718 VS4718 SR2516 SR 2516 survival Inhibitor SR-2516 cell VS 4718 inhibitor