BAY-876
目录号 : GC19061
BAY-876是一种选择性的葡萄糖转运蛋白1（GLUT1）抑制剂，IC50 为2nM。BAY-876 对GLUT2，GLUT3和 GLUT4 的IC50分别为10.8、1.67、0.29μM。
Cas No.:1799753-84-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines | SKOV-3, OVCAR-3, HEY , A2780 cells |
Preparation method | SKOV-3, OVCAR-3, HEY and A2780 cells were treated with BAY-876 (75nM) for 72 hours. |
Reaction Conditions | 75nM; 72h |
Applications | BAY-876 has growth inhibitory effects in SKOV-3, OVCAR-3 and HEY cells but not in A2780 cells. |
Animal experiment [2]: | |
Animal models | BalB/c mice |
Preparation method | MHCC97-H cells were cultured and injected into nude mice to form the subcutaneous tumor tissues. After MHCC97-H cells form tumor tissues in the subcutaneous position of nude mice, 5mg/kg BAY-876 was given by oral administration every day (once a day for two days). Then, the mice were analyzed by the micro-PET live imaging of small animals,and the tumor tissues were collected for the biochemical analysis. |
Dosage form | 5mg/kg; p.o. |
Applications | BAY-876 significantly inhibits tumor tissue formation and glucose uptake by cells in the tissue. |
References: | |
BAY-876 is a selective glucose transporter 1 (GLUT1) inhibitor with IC50 of 2 nM[1]. The IC50 of BAY-876 for GLUT2, GLUT3 and GLUT4 are 10.8, 1.67 and 0.29μM, respectively[1]. BAY-876 blocks glucose transport into tumor cells by inhibiting GLUT activity, thereby effectively inhibiting glucose uptake and tumor cell growth [2].
In vitro, BAY-876 (75nM) treated SKOV-3, OVCAR-3, HEY and A2780 cells for 72h and had a growth inhibitory effect on SKOV-3, OVCAR-3 and HEY cells, but not on A2780 cells [3] . BAY-876 (10 nM, 25 nM, 50 nM) treated CD4+ T cells and macrophages for 24 hours, significantly weakening the glucose uptake of cells and reducing the levels of inflammatory factors [4]. BAY-876 (10-1000µM) treated the renal adenocarcinoma 786-O cell line for 96 hours and significantly inhibited cell proliferation, with an IC50 of 53.56µM [5].
In vivo, BAY-876 (0, 1.5, 3.0, and 4.5 mg/kg/day) dose-dependently reduced tumor volume in NSG mice harboring SKOV-3 xenografts administered orally for 4 weeks and was effective in mice. Body weight has no effect [3]. BAY-876 (5 mg/kg/day) was administered orally for 2 days to mice bearing MHCC 97-H xenografts, which significantly inhibited tumor tissue formation and glucose uptake by cells in the tissue [6].
References:
[1] Siebeneicher H, Cleve A, Rehwinkel H, et al. Identification and optimization of the first highly selective GLUT1 inhibitor BAY‐876[J]. ChemMedChem, 2016, 11(20): 2261-2271.
[2] Kopitz C, Toschi L, Algire C, et al. Pharmacological characterization of BAY-876, a novel highly selective inhibitor of glucose transporter (GLUT)-1 in vitro and in vivo[J]. Cancer Research, 2016, 76(14_Supplement): 4746-4746.
[3] Ma Y, Wang W, Idowu M O, et al. Ovarian cancer relies on glucose transporter 1 to fuel glycolysis and growth: anti-tumor activity of BAY-876[J]. Cancers, 2018, 11(1): 33.
[4] Chen Z, Vaeth M, Eckstein M, et al. Characterization of the effect of the GLUT-1 inhibitor BAY-876 on T cells and macrophages[J]. European Journal of Pharmacology, 2023, 945: 175552.
[5] Peshraw Salih Hamadamin, et al. Exploring the anticancer potential of hydrogen sulfide and BAY 876 on clear cell renal cell carcinoma cells: Uncovering novel mutations in VHL and KDR genes among ccRCC patients[J]. Molecular and Clinical Oncology, 2024.
[6] Yang H, Zhang M Z, Sun H, et al. A novel microcrystalline BAY-876 formulation achieves long-acting antitumor activity against aerobic glycolysis and proliferation of hepatocellular carcinoma[J]. Frontiers in Oncology, 2021, 11: 783194.
BAY-876是一种选择性的葡萄糖转运蛋白1（GLUT1）抑制剂，IC50 为2nM[1]。BAY-876 对GLUT2，GLUT3和 GLUT4 的IC50分别为10.8、1.67、0.29μM[1]。BAY-876通过抑制GLUT活性，阻止葡萄糖转运进入肿瘤细胞，从而有效抑制葡萄糖摄取和肿瘤细胞生长[2]。
在体外，BAY-876（75nM）处理SKOV-3，OVCAR-3，HEY和A2780细胞72h，对SKOV-3，OVCAR-3和HEY细胞中具有生长抑制作用，但在A2780细胞中没有[3]。BAY-876（10 nM、25 nM、50 nM）处理CD4+ T细胞和巨噬细胞24h，显著减弱了细胞的葡萄糖摄取，且降低了炎症因子水平[4]。BAY-876（10-1000µM）处理肾腺癌786-O细胞系96h，显著抑制细胞增值，IC50为53.56µM[5]。
在体内，BAY-876（0、1.5、3.0和4.5 mg/kg/day）通过口服治疗携带SKOV-3异种移植物的NSG小鼠4周，剂量依赖性地减小了肿瘤体积，且对小鼠体重没有影响[3]。BAY-876（5 mg/kg/day）通过口服治疗携带MHCC 97-H异种移植物的小鼠2天，显著抑制了肿瘤组织生成和组织中细胞的葡萄糖摄取[6]。
| Cas No. | 1799753-84-6 | SDF | |
| Canonical SMILES | O=C(C1=NC2=CC(F)=CC=C2C(C(NC3=C(C)N(CC4=CC=C(C#N)C=C4)N=C3C(F)(F)F)=O)=C1)N | ||
| 分子式 | C24H16F4N6O2 | 分子量 | 496.42 |
| 溶解度 | DMSO : ≥ 100 mg/mL (201.44 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0144 mL | 10.0721 mL | 20.1442 mL |
| 5 mM | 0.4029 mL | 2.0144 mL | 4.0288 mL |
| 10 mM | 0.2014 mL | 1.0072 mL | 2.0144 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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