BAY-87-2243-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBAY 87-2243Cat. No.: HY-15836CAS No.: 1227158-85-1分式: CHFNO分量: 525.53作靶点: HIF/HIF Prolyl-Hydroxylase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 25 mg/mL (4

2、7.57 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.9028 mL 9.5142 mL 19.0284 mL5 mM 0.3806 mL 1.9028 mL 3.8057 mL10 mM 0.1903 mL 0.9514 mL 1.9028 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，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；

3、澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.76 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.76 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您边的抑制剂师www.MedChemE

4、物活性 BAY 87-2243种有效的选择性的 缺氧诱导因-1 (HIF-1) 抑制剂。IC50 & Target HIF-1 1体外研究 BAY 87-2243 inhibits luciferase activity with a calculated IC50 value of 0.7 nM. Hypoxic induction of the HIFtarget gene CA9 on protein level in HCT116luc cells is inhibited by BAY 87-2243 with an IC50 value of 2nM. BAY 87-2243 in

5、hibits mitochondrial oxygen consumption measured by using the oxygen sensitivefluorescence dye LUX-MitoXpress with an IC50 value of 10 nM 1. BAY-87-2243 inhibits nuclear HIF-1protein expression. Administration of BAY-87-2243 for about 18 days significantly reduces HIF-1 proteinexpression as well as

6、pimonidazole hypoxic fraction (pHF) (mean 2.4% (BAY-87-2243) vs. 17.6% (carrier), p2.体内研究 Nude mice are inoculated with H460 cells subcutaneously and after tumors have been established, animalsare treated with BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) for 3 weeks by daily oral gavage. BAY 87-2243reduced

7、tumor weight dose dependently in line with a dose-dependent reduction of the mRNA expressionlevels of the HIF-1 target genes CA9, ANGPTL4, and EGLN3, whereas the mRNA expression levels ofhypoxia-insensitive EGLN2 gene and of HIF-1 itself are not affected by compound treatment in vivo 1.PROTOCOLCell

8、Assay 1 Luciferase activity is given in % of DMSO-treated cells. To evaluate the cytotoxicity of BAY 87-2243, 2.000cells of the respective cell lines are seeded in 96-well plates and cultured in the appropriate growth mediumcontaining 10% FCS. BAY 87-2243 at various concentrations is added at 24 h a

9、fter seeding for additional 48h and cell viability is determined using Cell Titer Glow Assay 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 Tumor xenograft experiment is carried out on female immune-deficient, athymic NM

10、RI nude mice, aged 7-9weeks, weighing 20-25 g. The lung carcinoma xenograft mouse model is established by subcutaneousinjection into the right flank with 0.1 mL H460 tumor cells (1.5106) mixed 1:1 with Matrigel. Mice arerandomized into control and BAY 87-2243 (0.5, 1, 2, and 4 mg/kg) groups when tum

11、ors reach a size of morethan 40 mm2. Body weight is monitored as a measure for treatment-related, acute toxicity. Tumor area(measured by caliper) or tumor weight (measured when mice are sacrificed 21 days after cell injection) iscalculated by the formula 100-100(tumor weight/area of treatment group)

12、/(tumor weight/area of vehiclegroup). Tumor Statistical analysis is performed using the one-way analysis of variance.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Radiother Oncol. 2015 Sep;116(3):431-7. Cancer & Metabolism. 2019 Jul. Cance

13、r Metab. 2019 Mar 6;7:2. bioRxiv. 2019 Feb.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE bioRxiv. 2019 Jan.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ellinghaus P, et al. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitu

14、mor activities byinhibition of mitochondrial complex I. Cancer Med. 2013 Oct;2(5):611-24.2. Helbig L, et al. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionatedirradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep