GMB 475

Name: GMB 475
Brand: Tocris Bioscience
SKU: 7265

Tocris Bioscience, part of Bio-Techne | Catalog # 7265

COA / SDS

BCR-ABL1 kinase PROTAC® Degrader

Key Product Details

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)
Molecular Weight:	861.94

View Full Technical Details for GMB 475

Technical Data
Citations

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

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
E3 ligase	VHL
DC₅₀ / D_max	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

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 for GMB 475

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.16 mL	5.80 mL	11.60 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 Targeting BCR-ABL1 in chronic myeloid leukemia by PROTAC-mediated targeted protein degradation. Cancer Res 2019 PMID: 31311809