PND-1186
作者：齊岳
發布時間：2023-08-24
09:17:22
點擊數：
產品名稱：PND-1186
產品描述：
| 產品描述 | PND-1186 (VS-4718) is a reversible and specific FAK inhibitor (IC50: 1.5 nM). |
| 靶點活性 | FAK:1.5 nM |
| 體外活性 | 在負荷4T1腫瘤的小鼠體內,PND-1186（100 mg/kg,s.c.）可誘導細胞凋亡,對4T1皮下腫瘤生長產生抑制作用.在負荷ID8腫瘤的小鼠體內,PND-1186（0.5 mg/mL,p.o.）還會抑制卵巢癌腫瘤的生長. |
| 體內活性 | 在體外,PND-1186對4T1乳腺癌能動性有抑制作用,且可促進懸浮狀態的4T1凋亡,并使4T1軟瓊脂集落數量和大小減少。在HEY 和 OVCAR8細胞中,PND-1186促使G0-G1細胞周期阻滯,從而使細胞死亡。 |
| 激酶實驗 | 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. |
| 細胞實驗 | 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) |
| 別名 | SR-2516, PND 1186, VS-4718, PND1186 |
| 分子量 | 501.51 |
| 分子式 | C25H26F3N5O3 |
| CAS No. | 1061353-68-1 |
存儲
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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