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BAY 61-3606 dihydrochloride

Syk酪氨酸激酶抑制剂,BAY 61-3606 dihydrochloride 是一种有效的，选择性的，可逆的，ATP 竞争性的 Syk tyrosine kinase 抑制剂，IC50 值为 10 nM；对 Btk，Fyn，Itk，Lyn 和 Src 无抑制作用。

目录号: PC16020 纯度: ≥98%

CAS No. :648903-57-5

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中文名称	BAY 61-3606 dihydrochloride
中文别名	BAY-61-3606
英文名称	BAY 61-3606 dihydrochloride
英文别名	3-Pyridinecarboxamide,2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]-,dihydrochloride;2-[[7-(3,4-dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide,dihydrochloride;BAY 61-3606;BAY 61-3606 (dihydrochloride);BAY61-3606 dihydrochloride;BAY-61-3606;96PPV9GQ7A;2-((7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl)amino)nicotinamide dihydrochloride;C20H18N6O3.2ClH;HMS3746I13;BCP24726;3472AH;s7006;2-(7-(3,4-Dimethoxyphe;BAY 61-3606 dihydrochloride;2-(2-furanyl)benzonitrile;2-(2-Furyl)benzonitrile;648903-57-5 (HCl);BAY 61-3606 2HCl;BAY 61-3606 (dihydrochloride);BAY61-3606 dihydrochloride;BAY 61-3606;BAY 61-3606 hydrochloride;BAY 61-3606(dihydrochloride);bay 61-3606(hcl);BAY-613606;bay-61-3606 2hcl;BAY61-3606 dihydrochloride;BAY 61-3606;http:////www.amadischem.com/proen/548662/;http:////www.amadischem.com/proen/571789/
Cas No.	648903-57-5
分子式	C₂₀H₂₀Cl₂N₆O₃
分子量	463.32
包装储存	-20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

生物活性

BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a K_i 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.

性状

Solid

IC50 & Target[1][2]

Ki: 7.5 nM (Syk)
IC50: 10 nM (Syk)

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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

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)

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. [Information]

[2]. Tümmler C, et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells 体外研究. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

H₂O : 5 mg/mL (10.79 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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