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BAY 61-3606
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
BAY 61-3606图片
CAS NO:732983-37-8
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
BAY 61-3606 是一种有效的，具有口服活性的，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 降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化。BAY 61-3606 降低 K-rn 细胞裂解物中 Syk 磷酸化。Bay 61-3606 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 is an orally available, ATP-competitive, reversible and highly selectiveSykinhibitor with aKiof 7.5 nM and anIC50of 10 nM[1]. BAY 61-3606 reduces ERK1/2 andAktphosphorylation in neuroblastoma cell[2]. BAY 61-3606 induces a large decrease ofSykphosphorylation in K-rn cell lysates[3]. Bay 61-3606 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.

Western Blot Analysis[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.
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.
分子量

390.40

性状

Solid

Formula

C20H18N6O3

CAS 号

732983-37-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL(12.81 mM;ultrasonic and warming and heat to 80℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5615 mL12.8074 mL25.6148 mL
5 mM0.5123 mL2.5615 mL5.1230 mL
10 mM0.2561 mL1.2807 mL2.5615 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。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。