GMB-475 MedChemExpress (MCE)

Product Name	GMB-475
Synonyms	GMB-475 (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
CAS	2490599-18-1
EINECS
Chemical Formula	C43H46F3N7O7S
Molecular Weight	861.94
inchi
Package	1 mg;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	GMB-475 GMB-475 MedChemExpress (MCE) HY-125834 2490599-18-1 98.98% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US Descriptions GMB-475 GMB-475 MedChemExpress (MCE) HY-125834 2490599-18-1 98.98% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. 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)). GMB-475 (0.01-100 μM, 3 days) inhibits leukemic stem cell viability in chronic myeloid leukemia (CML) by targeting degradation of BCR-ABL1 protein kinase and inhibiting downstream STAT5 biomarkers[1]. GMB-475 (0-5 μM, 48 h) blocks multiple molecules in the JAK-STAT pathway, blocks the cell cycle and promotes apoptosis in Ba/F3 cells harboring the BCR::ABL1 mutant[2]. GMB-475 (5 mg/kg once every two days 10 days i.p.) improves chronic myeloid leukemia in mice with BCR::ABL1 mutant by targeted degradation of BCR-ABL1b and combined with dasatinib (HY-10181)[2]. STAT5 VHL Bcr-Abl \| \| \| \| \| \| \| \| \| \| [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. [Content Brief] [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. [Content Brief]
Last Update	2025-04-01 14:45:47

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