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说明： c-MET PROTAC®; also degrades exon-14-deleted c-MET
化学名： N-(3-Fluoro-4-((7-(3-(3-(3-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-3-oxopropoxy)propoxy)propoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
纯度： ≥98% (HPLC)
生物活性 for SJF 8240
SJF 8240 is a c-MET PROTAC® Degrader. Comprises MET inhibitor foretinib joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Degrades c-MET within 6 hours in vitro. Inhibits agonist-driven AKT phosphorylation and GTL16 cell proliferation (IC50 = 66.7 nM). Also degrades exon-14-deleted c-MET in Hs746T cells.
c-MET antibodies validated for Western Blot also available: Catalog # AF276 and MAB5694.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
技术数据 for SJF 8240
| 分子量 | 1106.25 |
| 公式 | C58H65F2N7O11S |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 2230821-68-6 |
| PubChem ID | 135175904 |
| InChI Key | SCUZPTNDZHEHLB-ZWUDBOSPSA-N |
| Smiles | COC1=CC2=C(N=CC=C2OC3=C(C=C(C=C3)NC(C4(C(NC5=CC=C(C=C5)F)=O)CC4)=O)F)C=C1OCCCOCCCOCCC(N[C@@H](C(C)(C)C)C(N6C[C@@H](C[C@H]6C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)O)=O)=O |
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 SJF 8240
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 55.31 | 50 |
制备储备液 for SJF 8240
以下数据基于产品分子量 1106.25。 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 |
|---|---|---|---|
| 0.5 mM | 1.81 mL | 9.04 mL | 18.08 mL |
| 2.5 mM | 0.36 mL | 1.81 mL | 3.62 mL |
| 5 mM | 0.18 mL | 0.9 mL | 1.81 mL |
| 25 mM | 0.04 mL | 0.18 mL | 0.36 mL |
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产品说明书 for SJF 8240
参考文献 for SJF 8240
参考文献是支持产品生物活性的出版物。
Burselem et al (2018) The advantages of targeted protein degradation over inhibition: an RTK case study. Cell Chem.Biol. 25 67 PMID: 29129716
If you know of a relevant reference for SJF 8240, please let us know.
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关键词: SJF 8240, SJF 8240 supplier, SJF8240, cmet, c-MET, degrades, MET, receptor, degraders, protacs, VHL, e3, ligase, targeted, protein, degradation, Receptors, Receptor, Degraders, 7266, Tocris Bioscience
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SJF 8240.
By
Povilas Kavaliauskas on 10/24/2023
分析类型： In Vitro
种属： Human
细胞系/组织： HSAEC1-Kt
We use this product to degrade the c-MET from HSAEC1-KT cells prior to infecting them with pathogenic fungi of our interest. We first performed a dose-response assay where we exposed the cells to different concentrations of SJF 8240 overnight in media containing 0.1% DMSO.
该领域的文献
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
TPD and Induced Proximity Research Product GuideUpdated
This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Assays for Protein Degradation
- Induced Proximity Tools
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia