PND-1186
作者：齐岳
发布时间：2023-08-24
09:17:22
点击数：
产品名称：PND-1186
产品描述：
| 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的小鼠体内,PND-1186（100 mg/kg,s.c.）可诱导细胞凋亡,对4T1皮下生长产生抑制作用.在负荷ID8的小鼠体内,PND-1186（0.5 mg/mL,p.o.）还会抑制卵巢*的生长. |
| 体内活性 | 在体外,PND-1186对4T1乳腺*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 | SR-2516, PND 1186, VS-4718, PND1186 |
| 分子量 | 501.51 |
| 分子式 | C25H26F3N5O3 |
| CAS No. | 1061353-68-1 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
H2O: <1 mg/mL
Ethanol: <1 mg/mL
DMSO: 23 mg/mL (45.9 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介绍：
西安齐岳生物科技有限公司是集化学科研和定制与一体的高科技化学公司。业务范围包括化学试剂和产品的研发、生产、销售等。涉及产品为通用试剂的分销、非通用试剂的定制与研发，涵盖生物科技、化学品、中间体和化工材料等领域。
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