PROTAC BCR-ABL1 ligand 1


Catalog No. Size PriceQuantity
M14388-2 Contact sales@xcessbio.com for quotation $100

Description

PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.

Product information

Molecular Weight: 347.29

Formula: C17H12F3N3O2

Chemical Name: 4-(6-{[4-(trifluoromethoxy)phenyl]amino}pyrimidin-4-yl)phenol

Smiles: OC1C=CC(=CC=1)C1C=C(NC2C=CC(=CC=2)OC(F)(F)F)N=CN=1

InChiKey: UNNHUSXTCNMGSB-UHFFFAOYSA-N

InChi: InChI=1S/C17H12F3N3O2/c18-17(19,20)25-14-7-3-12(4-8-14)23-16-9-15(21-10-22-16)11-1-5-13(24)6-2-11/h1-10,24H,(H,21,22,23)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GMB-475 (0-10 μM) exhibits cell proferation with IC50 values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively. GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells.

Products are for research use only. Not for human use.

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