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GMB 475

Cat. No. 7265 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： BCR-ABL1 kinase PROTAC® Degrader
化学名： (2S,4R)-1-((S)-3,3-Dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-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 (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 GMB 475

GMB 475 is a BCR-ABL1 kinase PROTAC® Degrader. Induces degradation of BCR-ABL1 and cABL1, inhibits downstream STAT5 signaling and suppresses cell proliferation in chronic myeloid leukemia cells lines.

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

技术数据 for GMB 475

E3 ligase VHL
DC50 / Dmax 340 nM / 95 (%) - Degradation of BCR-ABL in K562 cells after 18 h treatment
IC50 (Cellular activity) 1000-1110 nM - Inhibits proliferation of K562/BCR-ABL1 transformed Ba/F3 cells
Selectivity confirmed by global proteomics Yes
分子量 861.94
公式 C43H46F3N7O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 2490599-18-1
PubChem ID 139600282
InChI Key ONDVWISBMHHLGZ-SBJIGXGQSA-N
Smiles O=C(N[C@@H](C(C)(C)C)C(N1C[C@@H](C[C@H]1C(NCC2=CC=C(C3=C(N=CS3)C)C=C2)=O)O)=O)COCCOC4=CC=C(C5=CC(NC6=CC=C(OC(F)(F)F)C=C6)=NC=N5)C=C4

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 GMB 475

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 86.19 100

制备储备液 for GMB 475

以下数据基于产品分子量 861.94。 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 1.16 mL 5.8 mL 11.6 mL
5 mM 0.23 mL 1.16 mL 2.32 mL
10 mM 0.12 mL 0.58 mL 1.16 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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参考文献 for GMB 475

参考文献是支持产品生物活性的出版物。

Burslem et al (2019) Targeting BCR-ABL1 in chronic myeloid leukemia by PROTAC-mediated targeted protein degradation. Cancer Res 79 4744 PMID: 31311809

If you know of a relevant reference for GMB 475, please let us know.

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关键词: GMB 475, GMB 475 supplier, GMB475, PROTACs, Degraders, degrades, BCR-ABL1, tyrosine, kinase, CML, chronic, myeloid, leukemia, leukaemia, Abl, Kinase, 7265, 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 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