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GMB-475

GMB-475
GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein
Catalog No. T8488Cas No. 2490599-18-1
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GMB-475

Catalog No. T8488Cas No. 2490599-18-1

GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein
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Pack SizePriceAvailabilityQuantity
1 mg$88In Stock
5 mg$210In Stock
10 mg$369In Stock
25 mg$622In Stock
50 mg$885In Stock
100 mg$1,190In Stock
500 mg$2,430In Stock
1 mL x 10 mM (in DMSO)$289In Stock
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Product Introduction

Bioactivity
Description
GMB-475 is a BCR-ABL1 tyrosine kinase degrader based on PROTAC, overcoming BCR-ABL1-dependent drug resistance. GMB-475 targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel Lindau (VHL).resulting in ubiquitination and subsequent degradation of th
In vitro
GMB-475 inhibited the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitized Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.?Reverse phase protein array analysis suggested additional differences in levels of phosphorylated SHP2, GAB2, and SHC associated with BCR-ABL1 degradation.?Importantly, GMB-475 reduced viability and increased apoptosis in primary CML CD34+ cells, with no effect on healthy CD34+ cells at identical concentrations.?GMB-475 degraded BCR-ABL1 and reduced cell viability in primary CML stem cells.?Together, these findings suggest that combined BCR-ABL1 kinase inhibition and protein degradation may represent a strategy to address BCR-ABL1-dependent drug resistance, and warrant further investigation into the eradication of persistent leukemic stem cells, which rely on neither the presence nor the activity of the BCR-ABL1 protein for survival.
Chemical Properties
Molecular Weight861.93
FormulaC43H46F3N7O7S
Cas No.2490599-18-1
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 95 mg/mL (110.22 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1602 mL5.8009 mL11.6019 mL58.0094 mL
5 mM0.2320 mL1.1602 mL2.3204 mL11.6019 mL
10 mM0.1160 mL0.5801 mL1.1602 mL5.8009 mL
20 mM0.0580 mL0.2900 mL0.5801 mL2.9005 mL
50 mM0.0232 mL0.1160 mL0.2320 mL1.1602 mL
100 mM0.0116 mL0.0580 mL0.1160 mL0.5801 mL

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