BAY-826

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

BAY-826 

BAY-826 是有选择性的且有效的 TIE-2 抑制剂。BAY-826 的 Kd 值为 1.6 nM。

BAY-826

BAY-826 Chemical Structure

CAS No. : 1448316-08-2

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生物活性

BAY-826 is a selective and potent TIE-2 inhibitor with a Kd of 1.6 nM, respectively.

体外研究
(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.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

558.53

Formula

C26H19F5N6OS

CAS 号

1448316-08-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
  • [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.

Cell Assay

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

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] .

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [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.

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