GMB-475 是一种靶向蛋白水解的嵌合体(PROTAC)，它以变构方式靶向 BCR-ABL1 蛋白并募集 the E3 ligase Von Hippel-Lindau (VHL)，从而导致泛素化并随后降解致癌融合蛋白 Information GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. Targets BCR-ABL1 ; E3 ligase In vitro GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells. Cell Research(from reference) Cell lines：K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells) Concentrations：0.001-0.300 μM, 5 μM Incubation Time：3 days, 8 h
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GMB-475
CAS number：2490599-18-1 molecular formula：分子式:
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| Chinese alias | (2S,4R)-1-((S)-3,3-二甲基-2-(2-(2-(4-(6-((4-(三氟甲氧基)苯基)氨基)嘧啶-4-基)苯氧基)乙氧基)乙酰氨基)丁酰基)-4-羟基-N-(4-(4-甲基噻唑-5-基)苄基)吡咯烷-2-甲酰胺 | ||
| English alias | - | ||
| CAS number | 2490599-18-1 | molecular formula | 分子式: |
| molecular weight | 861.93 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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