PFK158
产品编号: DC10451
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应用领域
PFK-158 是一种有效的，选择性的 PFKFB3 抑制剂，IC50 值为 137 nM。PFK-158 可减少癌细胞中葡萄糖的摄取，ATP 的产生，乳酸的释放，并诱导细胞凋亡和自噬。PFK-158 具有广泛的抗肿瘤活性。PFK-158 还可以增强 Colistin 对细菌的抵抗力。
| Cas No.: |
1462249-75-7 |
| 名称: |
(E)-1-(pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one |
| 别名: |
PFK-158,PFK 158 |
| SMILES: |
O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2 |
| 分子式: |
C18H11F3N2O |
| 分子量: |
328.29 |
| 纯度: |
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| 保存条件: |
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: |
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| References: |
PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies. Target: PFKFB3 in vitro: PFK-158 is the first 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) inhibitor to undergo clinical trial testing in cancer patients. PFK-158, a small molecule therapeutic candidate that inactivates a novel cancer metabolism target never before examined in human clinical trials. PFK-158 is not only a first-in-class cancer drug but also the first to target glucose metabolism by inhibiting PFKFB3. PFK-158 is a nanomolar inhibitor of recombinant PFKFB3. PFK-158 inhibits PFKFB3 activity and glycolysis in cancer cells. in vivo: PFK158 is well tolerated in rats and dogs resulting in an acceptable pre-clinical therapeutic index. PFK158 is very effective in multiple preclinical mouse models of human-derived tumors and syngeneic murine models. IND-enabling safety and toxicity studies demonstrated that PFK158 is well tolerated in rats and dogs and supported the initiation of a phase I trial that is now underway. |
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MSDS
| TITLE |
DOWNLOAD |
| MSDS_219_DC10451_1462249-75-7 |
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COA
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DOWNLOAD |
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