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BAY 87-2243

Catalog No.
B1115
有效的HIF-1选择性抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 2,000.00
现货
10mg
¥ 1,240.00
现货
50mg
¥ 5,230.00
现货

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Background

BAY 87-2243 is a selective inhibitor of HIF-1 induced gene activation [1].

In HCT-116 cells, BAY 87-2243 inhibits the hypoxia increased HRE-dependent luciferase expression with IC50 value of 0.7nM and inhibits the expression of HIF target gene CA9 with IC50 value of 2nM. In H460 cells cultured under hypoxia, BAY 87-2243 suppresses the expression of HIF-1 target genes including CA9, adrenomedullin and angiopoietin-like protein-4. BAY 87-2243 also inhibits both HIF-1α and HIF-2α protein accumulation in this cell line. Moreover, in mice model bearing H460 xenograft, treatment of BAY 87-2243 reduces the expression levels of HIF-1 target genes CA9, ANGPTL4 and EGLN3 and meanwhile reduces the tumor weight. In addition, BAY 87-2243 is also found to act as an inhibitor of mitochondrial function. It can inhibit the oxygen consumption with IC50 value of 10nM [1].

References:
[1] Ellinghaus P, Heisler I, Unterschemmann K, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer medicine, 2013, 2(5): 611-624.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt525.53
Cas No.1227158-85-1
FormulaC26H26F3N7O2
Solubility≥8.76mg/mL in DMSO
Chemical Name5-(1-((2-(4-cyclopropylpiperazin-1-yl)pyridin-4-yl)methyl)-5-methyl-1H-pyrazol-3-yl)-3-(4-(trifluoromethoxy)phenyl)-1,2,4-oxadiazole
SDFDownload SDF
Canonical SMILESCC1=CC(C2=NC(C3=CC=C(OC(F)(F)F)C=C3)=NO2)=NN1CC4=CC=NC(N5CCN(C6CC6)CC5)=C4
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1, 2]:

细胞系

H460、RCC4细胞、BRAFWT 黑色素瘤细胞和BRAFV600E黑色素瘤细胞

溶解方法

有限的溶解度。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

1、10、100和1000 nmol/L BAY 87-2243给药处理16小时; 或10 nmol/L BAY 87-2243给药处理24、48和72 小时

应用

使用BAY 87-2243 (100 nmol/L)处理缺氧状态下的H460细胞,显著地抑制HIF靶基因(ANGPTL4, ADM和CA9)的表达;同时,BAY 87-2243抑制线粒体复合物I并且以剂量相关的方式诱导黑色素瘤细胞死亡。

动物实验 [1, 2]:

动物模型

H460肿瘤细胞异种移植模型; 黑色素瘤细胞(G-361和SK-MEL-28)异种移植模型; 人源衍生的黑色素瘤细胞(MEXF 276和MEXF 1732) 异种移植模型

剂量

0.5、1.0、2.0和4.0 mg/kg、口服给药、每日一次、持续21天; 或9 mg/kg、口服给药、每日一次

应用

BAY 87-2243以剂量相关的方式减少H460肿瘤重量且下调缺氧诱导因子蛋白及其靶基因的表达水平;同时BAY 87-2243显著地抑制所有包含BRAF突变黑色素瘤的生长。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Ellinghaus, P., Heisler, I., Unterschemmann, K., Haerter, M., Beck, H., Greschat, S., Ehrmann, A., Summer, H., Flamme, I., Oehme, F., Thierauch, K., Michels, M., Hess-Stumpp, H. and Ziegelbauer, K. (2013) BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer Med. 2, 611-624

2. Schockel, L., Glasauer, A., Basit, F., Bitschar, K., Truong, H., Erdmann, G., Algire, C., Hagebarth, A., Willems, P. H., Kopitz, C., Koopman, W. J. and Heroult, M. (2015) Targeting mitochondrial complex I using BAY 87-2243 reduces melanoma tumor growth. Cancer Metab. 3, 11

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