S86195 |
CBR-5884 |
| 源叶(MedMol) | 98% |
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- 产品描述： CBR-5884 是一种 phosphoglycerate dehydrogenase (PHGDH) 的选择性抑制剂，对应的IC50值为33 μM。CBR-5884 可抑制癌细胞中从头合成丝氨酸，并且对具有高丝氨酸生物合成活性的癌细胞具有选择性毒性
- 靶点： PHGDH(Cell-free assay):33 μM
- 体外研究：
CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. Biochemical characterization of the inhibitor reveals that it is a noncompetitive inhibitor that shows a time-dependent onset of inhibition and disrupts the oligomerization state of PHGDH
- 细胞实验： Cell lines: Carney cells Concentrations: 1 μM, 15 μM, 30 μM; 1 μM to 40 μM Incubation Time: 1 h; 3 h Method: Acute Toxicity Assay. Carney cells acclimated to growth in MEM media are plated in a 96-well plate at 6,000 cells per well. The next day, cells are treated with CBR-5884 from 1 μM to 40 μM for 3 h. Drug containing media are then removed, fresh drug-free media added, and cell viability is determined via a CellTiter-Glo or Alamar Blue assay according to the manufacturer’s protocol.
- 参考文献：
1. Edouard Mullarky, et al. Identification of a small molecule inhibitor of 3-phosphoglycerate dehydrogenase to target serine biosynthesis in cancers. Proc Natl Acad Sci U S A. 2016 Feb 16;113(7):1778-83.
- 溶解性： soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.973 ml 14.864 ml 29.728 ml 5 mM 0.595 ml 2.973 ml 5.946 ml 10 mM 0.297 ml 1.486 ml 2.973 ml 50 mM 0.059 ml 0.297 ml 0.595 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
