VS-4718 (PND-1186)

製品コードS7653 バッチS765303

印刷

化学情報

Chemical Structure Synonyms SR-2156 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H26F3N5O3
分子量 501.5 CAS No. 1061353-68-1
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.4 mM)
Ethanol 3 mg/mL (5.98 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 VS-4718 (PND-1186) is a reversible and selective FAK inhibitor with IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis. Phase 1.
in vitro VS-4718 (PND-1186) inhibits 4T1 breast carcinoma motility in vitro, promotes 4T1 apoptosis in suspended conditions, and decreases 4T1 soft agar colony number and size. [1] This compound also promotes G0-G1 cell-cycle arrest followed by cell death in HEY and OVCAR8 cells. [2]
in vivo In mice bearing 4T1 tumors, VS-4718 (PND-1186) (100 mg/kg s.c.) inhibits subcutaneous tumor growth by induction of apoptosis. It also causes ovarian carcinoma tumor growth inhibition in mice bearing ID8 tumors (0.5 mg/mL for p.o.). [1]

プロトコル(参考用のみ)

キナーゼアッセイ In vitro kinase activity
VS-4718 (PND-1186) is evaluated by measuring GST-FAK in vitro kinase activity and comparing it 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 for this compound 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.
細胞アッセイ 細胞株 Murine ID8 ovarian carcinoma cells
濃度 ~1 μM
反応時間 6 days
実験の流れ

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 VS-4718 (PND-1186) (final concentration for 0.6 mL). In separate experiments, this compound 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.
動物実験 動物モデル Mice bearing ID8 tumors or 4T1 tumors
投薬量 100 mg/kg every 12 hours for s.c.; 0.5 mg/mL for p.o.
投与方法 s.c. or p.o.

参考

  • https://pubmed.ncbi.nlm.nih.gov/20234191/
  • https://pubmed.ncbi.nlm.nih.gov/24899686/

カスタマーフィードバック

, , Cell Death Differ, 2017, 24(5):889-902

, , Oncogene, 2017, 36(39):5522-5531

Data from [Data independently produced by , , Molecular and Cellular Biology, 2016, 36(10):1555-1568.]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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