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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
|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|
|Storage||Store at -20°C|
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|
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.
|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|
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
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Citations for GMB 475
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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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
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