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GMB 475

Cat. No. 7265 Submit a Review Datasheet / COA / SDS
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Description: BCR-ABL1 kinase PROTAC® Degrader
Chemical Name: (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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity 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.

Technical Data 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
M. Wt 861.94
Formula C43H46F3N7O7S
Storage Store at -20°C
Purity ≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for GMB 475

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 86.19 100

Preparing Stock Solutions for GMB 475

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 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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References for GMB 475

References are publications that support the biological activity of the product.

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.

View Related Products by Target

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

Citations for GMB 475

Citations are publications that use Tocris products.

Currently there are no citations for GMB 475. Do you know of a great paper that uses GMB 475 from Tocris? Please let us know.

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Literature in this Area

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