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- 2025年07月23日
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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;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
BAY-826
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
1448316-08-2
- 规格：
25mg/10mg/5mg
| 规格： | 25mg | 产品价格： | ￥4590.0 |
|---|---|---|---|
| 规格： | 10mg | 产品价格： | ￥2090.0 |
| 规格： | 5mg | 产品价格： | ￥1190.0 |
| 基本信息 | |
| CAS | No.1448316-08-2 |
| 英文名称 | BAY-826 |
| 分子式 | C26H19F5N6OS |
| 分子量 | 558.53 |
| 溶解性 | Soluble in DMSO(Need ultrasonic) |
| 纯度 | ≥98% |
| 外观(性状) | Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| SMILES | CC1=CC(=C(C=C1NC(=O)C2=CC(=CC(=C2)C#N)S(F)(F)(F)(F)F)N3C=CN4C3=CC(=N4)C5=CN=CC=C5)C |
| InChIKey | MPASHPJAIUOWCK-UHFFFAOYSA-N |
| InChI | InChI=1S/C26H19F5N6OS/c1-16-8-17(2)24(36-6-7-37-25(36)13-23(35-37)19-4-3-5-33-15-19)12-22(16)34-26(38)20-9-18(14-32)10-21(11-20)39(27，28，29，30)31/h3-13，15H，1-2H3，(H，34，38) |
| PubChem CID | 71623052 |
| 靶点 | TIE-2 |
| 通路 | Protein Tyrosine Kinase/RTK |
| 背景说明 | BAY-826是有选择性的且有效的 TIE-2 抑制剂。 |
| 生物活性 | BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM， respectively.[1] |
| In Vitro | BAY-826 is a selective and potent inhibitor of TIE-2 (dissociation constant = 1.6 nM) and binds with similar high affinity to only 4 of 456 tested kinases， namely， TIE-1， DDR1， DDR2， and Serine/threonine-protein kinase 10 (LOK) (dissociation constant = 0.9， 0.4，1.3， and 5.9 nM).The high biochemical affinity for TIE-2 translates into very potent cellular mechanistic activity with an EC50 of about 1.3 nM for inhibition of TIE-2 autophosphorylation in human umbilical vein endothelial cells. The TIE-2 inhibitor BAY-826 is tested for its acute growth inhibitory as well as anti-clonogenic properties in all four mouse glioma cell lines. BAY-826 is highly selective against other angiogenic kinases， such as VEGFR， fibroblast growth factorreceptor (FGFR)， or Platelet-derived growth factor receptor (PDGFR)， and affects VEGF-stimulated proliferation of HUVEC only atμM concentrations， respectively.[1] |
| 细胞实验 | BAY-826 (oral gavage; 25 mg/kg，50 mg/kg，100 mg/k) potently inhibits ANG-1-stimulated TIE-2 autophosphorylation in murine lungs in female CB17/scid mice[1]. BAY-826 improves tumor control in syngeneic mouse glioma models. Co-treatment with BAY-826 and irradiation is ineffective in one model (SMA-497)， but provided synergistic prolongation of survival in another (SMA-560) cell. TIE- 2 inhibition may improve tumor response to treatment in highly vascularized tumors such as glioblastoma[1]. |
| 细胞实验 | Murine SMA-497， SMA-540， SMA-560， and GL-261 glioma cells are used.The cells are commonly cultured as adherent monolayers in Dulbecco`s modified Eagle medium supplemented with 10% heatinactivated fetal calf serum and 2 mM glutamine. Cells are irradiated in a Coradiation source at 1， 3， and 9 Gy. The cells are pre-incubated for 10 min in the 37°C incubator either with 0.1% DMSO as control or 1μM BAY-826. TIE-2 autophosphorylation is induced for 20 min with either 4 mM Na3VO4 or with 400 ng/mL COMP-ANG-1 in the presence of either 0.1% DMSO or 1 μM BAY-826[1]. |
| 动物实验 | Following anesthesia， a burr hole is drilled in the skull 2 mm lateral to the bregma. The needle of a Hamilton syringe is introduced to a depth of 3 mm. A volume of 2 μL of a single cell suspension in PBS is slowly injected into the right striatum. In female and male VM/Dk mice (in-house husbandry) 5×10 3 SMA glioma cells are implanted， whereas in female C57Bl/6 mice (Charles River) 2×104 GL-261 cells are implanted (n =10 per group). The mice employed have body weights >20 g. Systemic treatment with BAY-826 is performed by oral gavage (100 mg/kg body weight daily) or the solvent (10% Ethanol/40% Solutol/50% Aqua dest)， respectively [1] . |
| 数据来源文献 | [1]. Schneider H， et al. J Neurochem. 2017 Jan; 140(1):170-182. doi: 10.1111/jnc.13877. Epub 2016 Dec 12.Novel TIE-2 inhibitor BAY-826 displays in vivo efficacy in experimental syngeneic murine glioma models. |
| 单位 | 瓶 |
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