BAY 61-3606 dihydrochloride|cas:648903-57-5|西域试剂

BAY 61-3606 dihydrochloride,98.18%

产品编号：Bellancom-14985| CAS NO：648903-57-5| 分子式：C₂₀H₂₀Cl₂N₆O₃| 分子量：463.32

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货号	价格	库存与货期
Bellancom-14985	￥930.00	杭州北京（现货）
Bellancom-14985	￥1400.00	杭州北京（现货）
Bellancom-14985	￥2400.00	杭州北京（现货）
Bellancom-14985	￥9400.00	杭州北京（现货）

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BAY 61-3606 dihydrochloride

产品介绍

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，K_i 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 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^[4].

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.

西域 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^[4].

西域 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^[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.

体内研究

西域 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^[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.

体内研究

西域 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^[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.

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

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

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 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