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GMB 475

Catalog #: 7265 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7265/5
GMB 475 | CAS No. 2490599-18-1 | Active Degraders
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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%

Product Details
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Biological Activity

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

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
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2490599-18-1

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.

Product Datasheets

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