VS-4718 (PND-1186)

製品コードS7653 バッチS765306

印刷

化学情報

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）

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5mg/ml (9.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.25mg/ml (0.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <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
キナーゼアッセイ	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.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Chromosomal 3p loss and 8q gain drive vasculogenic mimicry via HIF-2α and VE-cadherin activation in uveal melanoma [ Cell Death Differ, 2025, 10.1038/s41418-025-01469-9]	PubMed: 40000790
Focal adhesion kinase plays an essential role in Th17 cell differentiation by stimulating NF-κB signaling [ Front Immunol, 2025, 16:1596802]	PubMed: 41050684
Exosomal Galectin-3 promotes peritoneal metastases in gastric adenocarcinoma via microenvironment alterations [ iScience, 2025, 28(1):111564]	PubMed: 39811647
The role of focal adhesion kinase in bladder cancer: translation from in vitro to ex vivo human urothelial carcinomas [ Radiol Oncol, 2025, 59(3):349-367]	PubMed: 40959921
Focal adhesion kinase-YAP signaling axis drives drug-tolerant persister cells and residual disease in lung cancer [ Nat Commun, 2024, 15(1):3741]	PubMed: 38702301
Focal adhesion kinase-YAP signaling axis drives drug-tolerant persister cells and residual disease in lung cancer [ Nat Commun, 2024, 15(1):3741]	PubMed: 38702301
Viral infection induces inflammatory signals that coordinate YAP regulation of dysplastic cells in lung alveoli [ J Clin Invest, 2024, 134(19)e176828]	PubMed: 39352385
Notochord segmentation in zebrafish controlled by iterative mechanical signaling [ Dev Cell, 2024, S1534-5807(24)00238-7]	PubMed: 38697108
Pivotal role of IL-8 derived from the interaction between osteosarcoma and tumor-associated macrophages in osteosarcoma growth and metastasis via the FAK pathway [ Cell Death Dis, 2024, 15(2):108]	PubMed: 38302407
Recycling machinery of integrin coupled with focal adhesion turnover via RAB11-UNC13D-FAK axis for migration of pancreatic cancer cells [ J Transl Med, 2024, 22(1):800]	PubMed: 39210440

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。