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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: 2-8℃，2 years
- 保质期：
Powder: 2-8℃，2 years
- 英文名：
BAY 61-3606
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
732983-37-8
- 规格：
5mg
| 基本信息 | |
| CAS | No.732983-37-8 |
| 英文名称 | BAY 61-3606 |
| 别名 | 2-[[7-(3，4-二C6H5OCH3基)咪唑并[1，2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺;Syk inhibitor IV |
| 分子式 | C20H18N6O3 |
| 分子量 | 390.4 |
| 溶解性 | Soluble in DMSO ≥0.1mg/mL(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder: 2-8℃，2 years |
| SMILES | COC1=C(C=C(C=C1)C2=CC3=NC=CN3C(=N2)NC4=C(C=CC=N4)C(=O)N)OC |
| InChIKey | JWQOJVOKBAAAAR-UHFFFAOYSA-N |
| InChI | InChI=1S/C20H18N6O3/c1-28-15-6-5-12(10-16(15)29-2)14-11-17-22-8-9-26(17)20(24-14)25-19-13(18(21)27)4-3-7-23-19/h3-11H，1-2H3，(H2，21，27)(H，23，24，25) |
| PubChem CID | 10200390 |
| 靶点 | Syk |
| 通路 | Protein Tyrosine Kinase/RTK |
| 背景说明 | BAY 61-3606是ATP竞争性，可逆的Syk选择性抑制剂，对Btk，Fyn，Itk，Lyn和Src无抑制性。 |
| 生物活性 | BAY 61-3606 is an orally available， ATP-competitive， reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM[1]. BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell[2]. BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates[3]. Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells[4]. |
| IC50 | Ki: 7.5 nM (Syk)[1].IC50: 10 nM (Syk)[1] |
| 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]. |
| 细胞实验 | 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]. |
| 数据来源文献 | [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. 2 [2]. Gioia R， et al. Quantitative phosphoproteomics revealed interplay between Syk and Lyn in the resistance to nilotinib in chronic myeloid leukemia cells. Blood. 2011 Aug 25;118(8):2211-21. [3]. Tümmler C， et al. SYK Inhibition Potentiates the Effect of Chemotherapeutic Drugs on Neuroblastoma Cells in Vitro. Cancers (Basel). 2019 Feb 10;11(2). pii: E202. [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. |
| 单位 | 瓶 |
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