货号	规格	价格	上海	北京	珠海	重庆	武汉
S89641-5mg买3赠1	99.10%	￥450.00 S89641-5mg ￥450.00 现货（买3赠1）	5 5	-	-	-	-
S89641-10mg买3赠1	99.10%	￥800.00 S89641-10mg ￥800.00 现货（买3赠1）	6 6	-	-	-	-
S89641-25mg促销	99.10%	￥1300.00 ￥1040.00 S89641-25mg ￥1040.00 现货	6 6	-	-	-	-
S89641-100mg促销	≥98%	￥3700.00 ￥2960.00 S89641-100mg ￥2960.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

Bcr-Abl

体外研究：

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.

体内研究：

GMB-475 (5 mg/kg; 每 2 天 1 次; 10 天; 腹腔注射) 通过靶向降解 BCR-ABL1b 并联合达沙替尼可用于改善小鼠 BCR::ABL1 突变体的慢性粒细胞白血病。

参考文献：

1. Burslem GM, et al. Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-mediated Targeted Protein Degradation. Cancer Res. 2019 Jul 16. pii: canres.1236.2019.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.16 ml	5.801 ml	11.602 ml
5 mM	0.232 ml	1.16 ml	2.32 ml
10 mM	0.116 ml	0.58 ml	1.16 ml
50 mM	0.023 ml	0.116 ml	0.232 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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GMB475

(2S)-1-((R)-3,3-dimethyl-2-(2-(2-(4-(6-((4-(trifluoromethoxy)phenyl)amino)pyrimidin-4-yl)phenoxy)ethoxy)acetamido)butanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)