Defactinib (VS-6063)

製品コードS7654 バッチS765406

印刷

化学情報

Synonyms

PF-04554878

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₂₁F₃N₈O₃S

分子量

510.49

CAS No.

1073154-85-4

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (195.89 mM)

Water

Insoluble

Ethanol

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.
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。	5.000mg/ml (9.79mM)	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 make it clear; 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.

* <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	Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.
in vitro	In taxane-sensitive (SKOV3ip1) and taxane-resistant (SKOV3-TR) cell lines, Defactinib (VS-6063) significantly inhibits pFAK (Tyr397) expression. The combination of this compound synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. ^[1] Its combination with Y15 also synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. ^[2]
in vivo	In both PTX-sensitive and PTX-resistant models, Defactinib (VS-6063) (50 mg/kg p.o.) enhances tumor growth inhibition. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells
	濃度	~10 μM
	反応時間	96 hours
	実験の流れ	Ovarian cancer cells are treated with increasing concentrations of Defactinib (VS-6063) for 96 hours and then subjected to the MTT assay. Results are confirmed with triplicate experiments.
動物実験	動物モデル	Mice bearing SKOV3ip1, SKOV3-TR, HeyA8 or HeyA8-MDR tumors
	投薬量	50 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/24062525/
https://pubmed.ncbi.nlm.nih.gov/25277206/

カスタマーフィードバック

: Data from [Data independently produced by , , Haematologica, 2018, 103(1):116-125]

: Data from [Data independently produced by , , Cell Death Differ. 2018, doi: 10.1038/s41418-018-0210-8]

: Data from [Data independently produced by , , Mol Cancer Ther, 2016, 15(9):2096-106]

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：

Epstein-Barr virus induces aberrant B cell migration and diapedesis via FAK-dependent chemotaxis pathways [ Nat Commun, 2025, 16(1):4581]	PubMed: 40389409
Role of the androgen receptor in melanoma aggressiveness [ Cell Death Dis, 2025, 16(1):34]	PubMed: 39837817
DIRAS3 Inhibits Ovarian Cancer Cell Growth by Blocking the Fibronectin-Mediated Integrin β1/FAK/AKT Signaling Pathway [ Cells, 2025, 14(16)1250]	PubMed: 40862729
Therapeutic benefit of the dual ALK/FAK inhibitor ESK440 in ALK-driven neuroblastoma [ Neoplasia, 2025, 60:100964]	PubMed: 39900433
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
A novel DNA repair protein, N-Myc downstream regulated gene 1 (NDRG1), links stromal tumour microenvironment to chemoresistance [ bioRxiv, 2025, 2025.01.22.634323]	PubMed: 39896456
FAK Drives Resistance to Therapy in HPV-Negative Head and Neck Cancer in a p53-Dependent Manner [ Clin Cancer Res, 2024, 30(1):187-197]	PubMed: 37819945
SPHK1 promotes bladder cancer metastasis via PD-L2/c-Src/FAK signaling cascade [ Cell Death Dis, 2024, 15(9):678]	PubMed: 39284838
Tumor microenvironment-induced FOXM1 regulates ovarian cancer stemness [ Cell Death Dis, 2024, 15(5):370]	PubMed: 38806454
ALK upregulates POSTN and WNT signaling to drive neuroblastoma [ Cell Rep, 2024, 43(3):113927]	PubMed: 38451815

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。