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SJF 0628

Cat. No. 7463 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent BRAF Degrader (PROTAC®
化学名： (2S,4R)-1-((S)-2-(2-(4-(4-(3-(2,6-Difluoro-3-(propylsulfonamido)benzoyl)-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
纯度： ≥98% (HPLC)
说明书
引用文献
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文献 (3)
生物活性 技术数据 溶解性 计算器 说明书 参考文献

生物活性 for SJF 0628

SJF 0628 is a potent, high affinity and mutant-selective Degrader (PROTAC®) of BRAF, comprising a ligand for the von Hippel Lindau E3 ligase joined by a piperazine linker to the BRAF kinase inhibitor vemurafenib. SJF 0628 induces degradation of all 3 classes of BRAF mutant in BRAF-dependent cancer cells without inducing degradation of the BRAFWT protein. The product degrades mutant BRAFV600E in BRAF-driven cancer cell lines (DC50 = 6.8 nM - 28 nM). SJ 0628 inhibits phosphorylation of MEK and ERK in SK-MEL-28 cells (DC50 = 10 nM) and inhibits cell growth in mutant-BRAF driven cancer cells (EC50 = 37 nM).

SJF 0661 negative control (Cat. No. 7464) and B-Raf antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF3424..

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

技术数据 for SJF 0628

分子量 1010.19
公式 C51H57F2N9O7S2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2413035-41-1
PubChem ID 146547699
InChI Key MBCAVOCJJAQHHT-FGUOTCRGSA-N
Smiles CCCS(=O)(NC1=CC=C(C(C(C2=CNC3=NC=C(C4=CC=C(N5CCN(CC5)CC(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)C=C4)C=C23)=O)=C1F)F)=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 0628

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 101.02 100

制备储备液 for SJF 0628

以下数据基于产品分子量 1010.19。 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.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
1 mM 0.99 mL 4.95 mL 9.9 mL
5 mM 0.2 mL 0.99 mL 1.98 mL
10 mM 0.1 mL 0.49 mL 0.99 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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产品说明书 for SJF 0628

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for SJF 0628

参考文献是支持产品生物活性的出版物。

Alabi et al (2021) Mutant-selective degradation by BRAF-targeting PROTACs. Nat.Commun. 12 PMID: 33568647

If you know of a relevant reference for SJF 0628, please let us know.

按标靶查看相关产品

关键词: SJF 0628, SJF 0628 supplier, SJF0628, BRAFV600E, kinase, inhibitors, degraders, PROTAC, degradation, raf, high, affinity, potent, Raf, Kinase, and, Ras, Degraders, 7463, Tocris Bioscience

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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。

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RAS Oncoproteins Scientific Review

RAS Oncoproteins Scientific Review

Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.

Targeted Protein Degradation Poster

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