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- PKD (Protein kinase D)
- GMB-475
GMB-475
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.
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包装价格促销价数量
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100mg￥0.000.00- +
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx13918
- CAS: 2490599-18-1
- 别名:
- 分子式: C43H46F3N7O7S
- 分子量: 861.93
- 纯度: ＞98%
- 溶解度: DMSO: 250 mg/mL (290.05 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
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.
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.[1]
[1] Burslem GM, et al. Cancer Res. 2019 Sep 15;79(18):4744-4753.
