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DD 03-171

Cat. No. 7160 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 BTK Degrader (PROTAC®)
化学名： 4-(1,1-Dimethylethyl)-N-[3-[6-[[4-[[4-[6-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]acetyl]amino]hexyl]-1-piperazinyl]carbonyl]phenyl]amino]-4,5-dihydro-4-methyl-5-oxo-2-pyrazinyl]-2-methylphenyl]benzamide
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)
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 DD 03-171

DD 03-171 is a potent and selective BTK Degrader (PROTAC®) (DC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

BTK antibodies validated for Western Blot also available: Catalog # MAB5807 and NBP2-02472.

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

许可信息

Sold under license from Dana-Farber Cancer Institute

技术数据 for DD 03-171

分子量 991.16
公式 C55H62N10O8
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2366132-45-6
PubChem ID 138059681
InChI Key QBPVFCNYKUENHU-UHFFFAOYSA-N
Smiles CN1C=C(N=C(NC2=CC=C(C=C2)C(=O)N2CCN(CCCCCCNC(=O)CNC3=C4C(=O)N(C5CCC(=O)NC5=O)C(=O)C4=CC=C3)CC2)C1=O)C1=C(C)C(NC(=O)C2=CC=C(C=C2)C(C)(C)C)=CC=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 DD 03-171

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 49.56 50

制备储备液 for DD 03-171

以下数据基于产品分子量 991.16。 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
0.5 mM 2.02 mL 10.09 mL 20.18 mL
2.5 mM 0.4 mL 2.02 mL 4.04 mL
5 mM 0.2 mL 1.01 mL 2.02 mL
25 mM 0.04 mL 0.2 mL 0.4 mL

Molarity Calculator

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参考文献 for DD 03-171

参考文献是支持产品生物活性的出版物。

Dobrovolsky et al (2019) Bruton tyrosine kinase degradation as a therapeutic strategy for cancer. Blood 133 952 PMID: 30545835

If you know of a relevant reference for DD 03-171, please let us know.

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关键词: DD 03-171, DD 03-171 supplier, DD03-171, Potent, selective, BTK, active, degraders, degrades, IKFZ1, IKFZ3, C481S-BTK, B-cell, malignancies, Bruton, tyrosine, kinase, PROTAC, PROTACs, targeted, protein, degradation, tpd, Brutons, Tyrosine, Kinase, (BTK), Degraders, 7160, 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。

TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

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

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