XY-06-007

Cat. No. 7669 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 and selective Degrader of Brd4^{BD1 L94V} fusion proteins

化学名： (2R)-2-((S)-6-(4-Chlorophenyl)-8-methoxy-1-methyl-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-(5-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetamido)pentyl)propanamide

纯度： ≥98% (HPLC)

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 XY-06-007

XY-06-007 is a highly selective and potent "Bump & Hole" TAG Degrader (DC_50,6h = 10 nM, T_1/2 < 43.2 min). XY-06-007 comprises a cereblon (CRBN) E3 ligase ligand joined by a linker to a (+)-JQ1 (Cat. No. 4499) derivative (the "bump" bearer) that selectively binds the Brd4^{BD1 L94V} variant (the "hole"). In cell lines expressing a fusion of the target protein with the tag, Brd4^{BD1 L94V}, XY-06-007 drives formation of a ternary complex between CRBN and the tagged protein, leading to ubiquitination and subsequent proteasomal degradation of the entire protein. XY-06-007 is highly selective for Brd4^{BD1 L94V} over wild-type, and is broadly selective across the proteome. XY-06-007 can be combined with the dTAG approach to achieve simultaneous degrader-mediated depletion of their respective protein fusions. XY-06-007 is suitable for in vivo studies.

许可信息

Sold under license from Dana-Farber Cancer Institute

技术数据 for XY-06-007

分子量	809.28
公式	C₄₁H₄₁ClN₈O₈
储存	Store at -20°C
纯度	≥98% (HPLC)
CAS Number	2757045-94-4
PubChem ID	162526515
InChI Key	QTDHGBJLMBQHOW-BPJPHOPQSA-N
Smiles	COC1=CC=C(C2=C1)N3C([C@H]([C@@H](C)C(NCCCCCNC(COC4=CC=CC(C(N5C6C(NC(CC6)=O)=O)=O)=C4C5=O)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C

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 XY-06-007

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	80.93	100

制备储备液 for XY-06-007

以下数据基于产品分子量 809.28。 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	1.24 mL	6.18 mL	12.36 mL
5 mM	0.25 mL	1.24 mL	2.47 mL
10 mM	0.12 mL	0.62 mL	1.24 mL
50 mM	0.02 mL	0.12 mL	0.25 mL

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产品说明书 for XY-06-007

分析证书/产品说明书

化学品安全技术说明书

参考文献 for XY-06-007

参考文献是支持产品生物活性的出版物。

Nowak et al (2021) Structure-guided design of a "Bump-and-Hole" Bromodomain-based degradation tag. J.Med.Chem. 64 11637 PMID: 34279939

If you know of a relevant reference for XY-06-007, please let us know.

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关键词: XY-06-007, XY-06-007 supplier, XY06007, TAG, Degrades, Degraders, degradation, targets, fusion, proteins, BromoTag, Brd4BD1L94V, Degradation, Platform, 7669, 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!

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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

Validating Targets for TPD Using dTAG Poster

The dTAG platform offers a generalizable strategy to degrade, in principle, any intracellular protein of interest (POI) and is a useful strategy for exploration and validation of targets. This poster presents a workflow solution for target validation, from custom TAG knock-in cell-lines for your POI, different dTAG Degraders to knockdown you POI, to automated assays for protein degradation using Simple Western^TM instruments. Data are also presented on the use of an antibody that recognizes the TAG domain (FKBP12^F36V) for detection of degradation. Presented at TPD Europe, March 2022, London, UK.