规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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体外研究 (In Vitro) |
BAY 87-2243 抑制荧光素酶活性,IC50 值约为 0.7 nM。 BAY 87-2243 在 HCT116luc 细胞的蛋白质水平上抑制 HIF 靶基因 CA9 的缺氧表达,IC50 值约为 2 nM。根据氧敏感荧光染料 LUX-MitoXpress[1] 的测定,BAY 87-2243 的 IC50 值小于 10 nM,可抑制线粒体耗氧量。 BAY-87-2243 抑制核 HIF-1α 蛋白表达。与相对血管面积 (RVA) 和灌注血管 (PF) 相比,BAY-87-2243 给药约 18 天可显着降低 HIF-1α 蛋白表达、坏死分数 (NF)(平均 9% vs. 35.6%,p =0.0002) 和哌莫硝唑缺氧分数 (pHF)(平均 2.4% (BAY-87-2243) 对比 17.6%(载体),p<0.0001)[2]。
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体内研究 (In Vivo) |
将 H460 细胞皮下注射到裸鼠体内,一旦肿瘤形成,小鼠每天接受 BAY 87-2243(0.5、1、2 和 4 mg/kg)口服灌胃治疗,持续三周。根据 HIF-1 靶基因 CA9、ANGPTL4 和 EGLN3 mRNA 表达水平的剂量依赖性降低,BAY 87-2243 降低了肿瘤重量。然而,体内化合物治疗对缺氧不敏感的EGLN2基因或HIF-1α本身的mRNA表达水平没有影响[1]。
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动物实验 |
Mice bearing lung carcinoma H460 xenografts;
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参考文献 |
[1]. Ellinghaus P, 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 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 fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep 19;9:207 |
分子式 |
C26H26F3N7O2
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分子量 |
525.5256
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CAS号 |
1227158-85-1
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相关CAS号 |
1227158-85-1
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SMILES |
FC(OC1C([H])=C([H])C(=C([H])C=1[H])C1=NOC(C2C([H])=C(C([H])([H])[H])N(C([H])([H])C3C([H])=C([H])N=C(C=3[H])N3C([H])([H])C([H])([H])N(C([H])([H])C3([H])[H])C3([H])C([H])([H])C3([H])[H])N=2)=N1)(F)F
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InChi Key |
CDJNNOJINJAXPV-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3
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化学名 |
1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-piperazine
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别名 |
BAY-872243; BAY 872243; BAY-872243; BAY-87-2243; BAY87-2243; BAY 87-2243
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO:<1 mg/mL
Water:<1 mg/mL
Ethanol: 8 mg/mL(15.22 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.76 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9028 mL | 9.5142 mL | 19.0284 mL | |
5 mM | 0.3806 mL | 1.9028 mL | 3.8057 mL | |
10 mM | 0.1903 mL | 0.9514 mL | 1.9028 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01297530 | Terminated | Drug: BAY87-2243 | Neoplasms | Bayer | April 2011 | Phase 1 |
(A) Chemical structure of BAY 87-2243. (B) BAY 87-2243 suppresses hypoxia-induced reporter gene activity (left), and CA9 protein levels in vitro in HCT-116 cell lysates (right). Cancer Med. 2013 Oct;2(5):611-24. td> |
BAY 87-2243 is inactive in RCC4 cells lacking functional VHL protein or in H460 cells silenced for EGLN1.Cancer Med.2013 Oct;2(5):611-24. td> |
BAY 87-2243 reduces tumor weight, hypoxia-inducible factor (HIF)-1α protein levels, and HIF-1 target gene expression in H460 xenograft tumors. Cancer Med. 2013 Oct;2(5):611-24. td> |