Defactinib (VS-6063)

製品コードS7654 バッチS765404

印刷

化学情報

Chemical Structure 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 100 mg/mL warmed with 50ºC water bath (195.89 mM)
Water Insoluble
Ethanol Insoluble
* <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, VS-6063 significantly inhibits pFAK (Tyr397) expression. The combination of VS-6063 and paclitaxel synergistically decreases proliferation and increases apoptosis in SKOV3ip1, SKOV3-TR, HeyA8 and HeyA8-MDR cells. [1] The combination of VS-6063 and Y15 synergistically decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines. [2]
in vivo In both PTX-sensitive and PTX-resistant models, VS-6063 (50 mg/kg p.o.) enhances tumor growth inhibition by paclitaxel. [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 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.

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：

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
ALK upregulates POSTN and WNT signaling to drive neuroblastoma [ Cell Rep, 2024, 43(3):113927] PubMed: 38451815
Histone deacetylase inhibitors promote breast cancer metastasis by elevating NEDD9 expression [ Signal Transduct Target Ther, 2023, 8(1):11] PubMed: 36604412
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, gutjnl-2022-327927] PubMed: 36977556
FAK suppresses antigen processing and presentation to promote immune evasion in pancreatic cancer [ Gut, 2023, 1–2] PubMed: None
Epigenetic suppression of PGC1α (PPARGC1A) causes collateral sensitivity to HMGCR-inhibitors within BRAF-treatment resistant melanomas [ Nat Commun, 2023, 14(1):3251] PubMed: 37277330
GSNOR deficiency promotes tumor growth via FAK1 S-nitrosylation [ Cell Rep, 2023, 42(1):111997] PubMed: 36656716
FAK-mediated phosphorylation at Y464 regulates p85β nuclear translocation to promote tumorigenesis of ccRCC by repressing RB1 expression [ Cell Rep, 2023, 42(3):112188] PubMed: 36857183
FTO facilitates cancer metastasis by modifying the m6A level of FAP to induce integrin/FAK signaling in non-small cell lung cancer [ Cell Commun Signal, 2023, 10.1186/s12964-023-01343-6] PubMed: 37919739
Developing SHP2-based combination therapy for KRAS-amplified cancer [ JCI Insight, 2023, 8(3)e152714] PubMed: 36752207

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。