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Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $88 | In Stock | |
5 mg | $210 | In Stock | |
10 mg | $369 | In Stock | |
25 mg | $622 | In Stock | |
50 mg | $885 | In Stock | |
100 mg | $1,190 | In Stock | |
500 mg | $2,430 | In Stock | |
1 mL x 10 mM (in DMSO) | $289 | In Stock |
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. |
Molecular Weight | 861.93 |
Formula | C43H46F3N7O7S |
Cas No. | 2490599-18-1 |
Storage | store 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
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