| 产品描述： | BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM. BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells |
| 靶点： |
Ki: 7.5 nM (Syk) IC50: 10 nM (Syk);Apoptosis; Syk |
| 体外研究： |
BAY 61-3606 (0.01-10 μM ; 48 hours) significantly reduces the cell viability of SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells in a dose-dependent matter. SH-SY5Y cells expressing high SYK levels are significantly more sensitive to BAY 61-3606 in comparison to SK-N-BEcells expressing very low or no SYK. BAY 61-3606 (0.4 and 0.8 μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y. BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates. Cell Viability Assay Cell Line: SYK-positive SH-SY5Y and SYK-negative SK-N-BE cells Concentration: 0.01, 0.1, 1, and 10 μM Incubation Time: 48 hours Result: Significantly reduced the cell viability of both cell lines in a dose-dependent matter. Cell Proliferation Assay Cell Line: SH-SY5Y cells Concentration: 0.4 and 0.8 μM Incubation Time: 4 or 24 hours Result: Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24 h treatment. Western Blot Analysis Cell Line: K-rn cell lysates Concentration: 2 μM Incubation Time: 2 hours Result: Induced a large decrease of Syk phosphorylation. |
| 体内研究： |
Bay 61-3606 (50 mg/kg; administered twice a week for two weeks by intraperitoneal injection) alone leads to more efficacious reductions than that of TNF-related apoptosis-inducing ligand (TRAIL; 10 mg/kg) alone in MCF-7 tumor xenograft-bearing BALB/c nude mice. Bay 61-3606 administered in TRAIL combination significantly reduces the volume of the xenografted tumor. Animal Model: Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograftDosage: 50 mg/kg Administration: Injected intraperitoneally twice a week with Bay 61–3606 (50 mg/kg), TRAIL (10 mg/kg) or a combination of Bay 61-3606 (50 mg/kg) and TRAIL (10 mg/kg); TRAIL was given 2 h after the injection of Bay 61-3606; for two weeks Result: Led to efficacious reductions in tumor growth. |
| 参考文献： |
1. Yamamoto N, et al. The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents. J Pharmacol Exp Ther. 2003 Sep;306(3):1174-81. 2. Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. 3. Gioia R, et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to AMN107 in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. 4. Kim SY, et al. Bay 61-3606 Sensitizes TRAIL-Induced Apoptosis by Downregulating Mcl-1 in Breast Cancer Cells. PLoS One. 2015 Dec 31;10(12):e0146073. |
| 溶解性： |
Soluble in H2O |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.562 ml |
12.808 ml |
25.615 ml |
| 5 mM |
0.512 ml |
2.562 ml |
5.123 ml |
| 10 mM |
0.256 ml |
1.281 ml |
2.562 ml |
| 50 mM |
0.051 ml |
0.256 ml |
0.512 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京