BAY 61-3606 2HCL - CAS:648903-57-5 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	BAY 61-3606 2HCL
英文名称:	BAY 61-3606 2HCL
别名:	BAY613606;2-((7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl)amino)nicotinamide 2HCL
CAS No:	648903-57-5	分子式:	C₂₀H₂₀Cl₂N₆O₃	分子量:	463.32
CAS No:	648903-57-5
分子式:	C₂₀H₂₀Cl₂N₆O₃
分子量:	463.32

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

B10418 BAY 61-3606 2HCL ≥98% (psaitong)

相关产品

包装规格：

5mg 10mg 50mg in glass bottle

溶解性：

溶于DMSO

产品描述：

基本信息

产品编号：B10418
产品名称：BAY 61-3606 2HCL
CAS:	648903-57-5	储存条件	粉末	-20℃	四年

分子式：	C20H20Cl2N6O3		溶于液体	-80℃	六个月
分子量	463.32			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	14mg/mL (30.21mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.1583mL	10.7917mL	21.5834mL
5mM	0.4317mL	2.1583mL	4.3167mL
10mM	0.4317mL	2.1583mL	4.3167mL

生物活性

产品描述	一种口服有效的，ATP 竞争性的，可逆的选择性Syk抑制剂。
靶点/IC₅₀	Ki: 7.5nM (Syk) IC50: 10nM (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 0.8μM; 4 or 24 hours) inhibits SYK activity by reducing ERK1/2 and Akt phosphorylation in neuroblastoma cell SH-SY5Y.BAY 61-3606(2μM; 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 10μM
	Incubation Time:	48 hours
	Result:	Significantly reduced the cell viability of both cell lines in a dose-dependent matter.
	Western Blot Analysis
	Cell Line:	SH-SY5Y cells
	Concentration:	0.4 and 0.8μM
	Incubation Time:	4 or 24 hours
	Result:	Reduced the phosphorylation of ERK1/2 and Akt after a 4 or 24h treatment.
	Western Blot Analysis
	Cell Line:	K-rn cell lysates
	Concentration:	2μM
	Incubation Time:	2 hours
	Result:	Induced a large decrease of Syk phosphorylation.
体内研究	Bay 61-3606 (50mg/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; 10mg/kg) alone in MCF-7 tumor xenograftbearing 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:	50mg/kg
	Administration:	Injected intraperitoneally twice a week with Bay 61-3606 (50mg/kg), TRAIL (10mg/kg) or a combination of Bay 61-3606 (50mg/kg) and TRAIL (10mg/kg); TRAIL was given 2h after the injection of Bay 61-3606; for two weeks
	Result:	Led to efficacious reductions in tumor growth.

推荐实验方法(仅供参考)

细胞实验:
细胞系	MCF-7细胞
浓度	2.5μM或5μM
处理时间	12h或24h
方法	将MCF-7细胞暴露于TRAIL（0, 12.5, 25, 37.5ng/ml），加入或不加入Bay 61-3606 (2.5μM)，培养24小时。暴露于这些试剂12小时后，用活性Bak抗体对这些细胞进行免疫细胞化学分析；用5μM Bay 61-3606处理MCF-7细胞，加入或不加入TRAIL (50ng/ml)处理24小时，测定Caspase的活性。