GMB-475
规格
| Cas Number | 2490599-18-1 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 别名 | (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 |
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL (116.01 mM); Ethanol: 50 mg/mL (58.0 mM); Water: Insoluble; |
| 简短描述 | 普罗塔克 |
| 英文简短描述 | PROTAC |
| 过滤标签 | 羟基聚乙二醇,PROTACs,Bcr-Abl,Protein Tyrosine Kinase/RTK,PROTAC,PROTAC linker,DBCO PEG,Aliphatic Linkers |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | GMB-475 是一种蛋白水解靶向嵌合体 (PROTAC)，可异位靶向 BCR-ABL1 蛋白，并招募 E3 连接酶 Von Hippel-Lindau (VHL)，导致泛素化，进而降解致癌融合蛋白。 |
| 描述 |
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 |
| 英文描述 |
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 |