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说明： Potent and selective FAK and Pyk2 inhibitor
化学名： N-Methyl-4-[[4-[[[3-[methyl(methylsulfonyl)amino]-2-pyrazinyl]methyl]amino]-5-(trifluoromethyl)-2-pyrimidinyl]amino]benzamide
纯度： ≥98% (HPLC)
生物活性 for Defactinib
Defactinib is a potent and selective focal adhesion kinase (FAK) and proline rich tyrosine kinase 2 (Pyk2) inhibitor (IC50 = 0.6 nM at both). The compound shows >100-fold selectivity for FAK and Pyk2 over other kinases. Defactinib inhibits FAK phosphorylation in vivo (EC50 = 26 nM), and inhibits tumor growth. Defactinib also decreases the viability of thyroid cancer cells, showing greater selectivity for TT and K1 cells compared to FAK Inhibitor 14 (Cat. No. 3414) (IC50 values are 1.98 μM and 10.34 μM, respectively). Defactinib suppresses colony growth of Pnf cells when combined with Selumetinib (Cat. No. 6815).
许可信息
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the Defactinib (PF-04554878) probe summary on the SGC website.
化合物库 for Defactinib
Defactinib is also offered as part of the Tocriscreen Kinase Inhibitor Library. 了解 Tocris 化合物库的更多信息。
技术数据 for Defactinib
| 分子量 | 510.49 |
| 公式 | C20H21F3N8O3S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1073154-85-4 |
| PubChem ID | 25117126 |
| InChI Key | FWLMVFUGMHIOAA-UHFFFAOYSA-N |
| Smiles | CNC(=O)C1=CC=C(NC2=NC=C(C(NCC3=NC=CN=C3N(C)[S](C)(=O)=O)=N2)C(F)(F)F)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for Defactinib
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 51.05 | 100 |
制备储备液 for Defactinib
以下数据基于产品分子量 510.49。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.96 mL | 9.79 mL | 19.59 mL |
| 5 mM | 0.39 mL | 1.96 mL | 3.92 mL |
| 10 mM | 0.2 mL | 0.98 mL | 1.96 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.39 mL |
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产品说明书 for Defactinib
参考文献 for Defactinib
参考文献是支持产品生物活性的出版物。
Jones et al (2015) A phase I study of VS-6063, a second-generation focal adhesion kinase inhibitor, in patients with advanced solid tumors. Invest. New Drugs 33 1100 PMID: 26334219
O'Brien et al (2014) FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics. Oncotarget. 5 7945 PMID: 25277206
Errico et al (2021) Neurofibromin deficiency and extracellular matrix cooperate to increase transforming potential through FAK-dependent signaling. Cancers 13 PMID: 34066061
If you know of a relevant reference for Defactinib, please let us know.
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关键词: Defactinib, Defactinib supplier, vs6063, PF04554878, potent, selective, inhibitors, focal, adhesion, kinases, FAK, Pyk2, SGC, PTK, PTK2B, Focal, Adhesion, Kinase, 7305, Tocris Bioscience
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