GMB-475 NEW
| Price | $88 | $210 | $369 |
| Package | 1mg | 5mg | 10mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-18 |
Product Details
| Product Name: GMB-475 | CAS No.: 2490599-18-1 |
| Purity: 98.78% | Supply Ability: 10g |
| Release date: 2024/11/18 |
Product Introduction
Bioactivity
| 名稱 | GMB-475 |
| 描述 | 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 |
| 體外活性 | 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. |
| 存儲(chǔ)條件 | 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. |
| 溶解度 | DMSO : 95 mg/mL (110.22 mM), Sonication is recommended. |
| 關(guān)鍵字 | Bcr-Abl | PROTACs | GMB-475 | Apoptosis | Inhibitor | inhibit | GMB475 | GMB 475 |
| 相關(guān)產(chǎn)品 | Imatinib Mesylate | ARV-471 | Dasatinib | GNF-5 | dBET6 | Ponatinib | Nilotinib monohydrochloride monohydrate | Nilotinib | Imatinib | Masitinib |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 泛素化化合物庫(kù) | 激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 血管生成庫(kù) | NO PAINS 化合物庫(kù) | 已知活性化合物庫(kù) | 細(xì)胞骨架化合物庫(kù) | 抗癌化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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United States- Since: 2011-01-07
- Address: 36?Washington?Street, Wellesley?Hills
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