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• 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 xenograft Dosage: 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	2.158 ml	10.792 ml	21.583 ml
  5 mM	0.432 ml	2.158 ml	4.317 ml
  10 mM	0.216 ml	1.079 ml	2.158 ml
  50 mM	0.043 ml	0.216 ml	0.432 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

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

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *