GMB-475

CAT: 0804-HY-125834-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-125834-01Size:5 mg
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Description
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].
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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Bcr-Abl; STAT5; von Hippel-Lindau (VHL)

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