GMB-475

GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL) . GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845) ; Black: Linker; Pink: BCR-ABL1 ligand (HY-11007) ) [1][2].

Product Specifications

CAS Number

[2490599-18-1]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Bcr-Abl; JAK; PROTACs; STAT

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; PROTAC; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/gmb-475.html

Concentration

10mM

Purity

98.69

Solubility

DMSO : 250 mg/mL (ultrasonic)

Smiles

FC(F)(F)OC1=CC=C(NC2=CC(C3=CC=C(OCCOCC(N[C@@H](C(C)(C)C)C(N4[C@H](C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)=O)C=C3)=NC=N2)C=C1

Molecular Formula

C43H46F3N7O7S

Molecular Weight

861.93

Precautions

H302, H315, H319, H335

References & Citations

[1]Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation. Cancer Res. 2019 Sep 15;79 (18) :4744-4753. |[2]Ye W, et al. The proteolysis targeting chimera GMB-475 combined with dasatinib for the treatment of chronic myeloid leukemia with BCR::ABL1 mutants. Front Pharmacol. 2022 Oct 3;13:931772.