BAY 61-3606 dihydrochloride 是一种口服有效的,ATP 竞争性的,可逆的选择性Syk抑制剂,Ki为 7.5 nM,IC50为 10 nM。BAY 61-3606 dihydrochloride 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 dihydrochloride 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 dihydrochloride 作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。
生物活性 | BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selectiveSykinhibitor with aKiof 7.5 nM anIC50of 10 nM[1]. BAY 61-3606 dihydrochloride reduces ERK1/2 andAktphosphorylation in neuroblastoma cell[2]. BAY 61-3606 dihydrochloride induces a large decrease ofSykphosphorylation in K-rn cell lysates[3]. Bay 61-3606 dihydrochloride sensitizes TRAIL-inducedapoptosisby downregulatingMcl-1in breastcancercells[4]. |
IC50& Target | Ki: 7.5 nM (Syk)[1] IC50: 10 nM (Syk)[1] |
体外研究 (In Vitro) | 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[2]. 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[2]. BAY 61-3606 (2 μM; 2 hours) induces a large decrease of Syk phosphorylation in K-rn cell lysates[3].
Cell Viability Assay[2] 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[2] 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[3] Cell Line: | K-rn cell lysates | Concentration: | 2 μM | Incubation Time: | 2 hours | Result: | Induced a large decrease of Syk phosphorylation. |
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体内研究 (In Vivo) | 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[4].
Animal Model: | Female BALB/c nude mice (5 weeks old) bearing MCF-7 tumor xenograft[4] | 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 5 mg/mL(10.79 mM;Need ultrasonic) 配制储备液 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL | 5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL | 10 mM | 0.2158 mL | 1.0792 mL | 2.1583 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution
此方案可获得 ≥ 0.71 mg/mL (1.53 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 0.71 mg/mL (1.53 mM); Clear solution
此方案可获得 ≥ 0.71 mg/mL (1.53 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 7.1 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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