PFK-158
CAS No. 1462249-75-7
PFK-158 ( PFK158 | PFK 158 | PFK158 | ACTPFK158 )
产品货号. M17311 CAS No. 1462249-75-7
PFK-158 是一种有效且特异性的 PFKFB3 抑制剂。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 5MG | ¥594 | 有现货 |
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| 10MG | ¥947 | 有现货 |
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| 25MG | ¥1683 | 有现货 |
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| 50MG | ¥2632 | 有现货 |
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| 100MG | ¥3762 | 有现货 |
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| 200MG | ¥5373 | 有现货 |
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| 500MG | 获取报价 | 有现货 |
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| 1G | 获取报价 | 有现货 |
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| 1 mL x 10 mM in DMSO | ¥454 | 有现货 |
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生物学信息
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产品名称PFK-158
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述PFK-158 是一种有效且特异性的 PFKFB3 抑制剂。
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产品描述PFK-158, also known as ACT-PFK-158, is an inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) with potential antineoplastic activity. Upon administration, PFKFB3 inhibitor PFK-158 binds to and inhibits the activity of PFKFB3, which leads to the inhibition of both the glycolytic pathway in and glucose uptake by cancer cells. This prevents the production of macromolecules and energy that causes the enhanced cellular proliferation in cancer cells as compared to that of normal, healthy cells. Depriving cancer cells of nutrients and energy leads to the inhibition of cancer cell growth.(In Vitro):PFK-158 (10 μM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%).PFK-158 (0-10 μM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively.PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs.(In Vivo):PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model.
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体外实验PFK-158 (10 μM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%).PFK-158 (0-10 μM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively.PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs. Apoptosis Analysis Cell Line: OV2008 and C13 cells Concentration:10 μM Incubation Time:24 hours Result:Combined with Carboplatin (CBPt) treatment resulted in significant increase in apoptosis.Western Blot Analysis Cell Line:C13 and HeyA8MDR cells Concentration:0 μM, 5 μM, 10 μM Incubation Time:24 hours Result:Demonstrated a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.
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体内实验PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model. Animal Model:Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells Dosage:15 mg/kg Administration:Intraperitoneal injection; once a week; for 4 weeks Result:A marked reduction of tumor growth was observed in the combination treatment.
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同义词PFK158 | PFK 158 | PFK158 | ACTPFK158
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通路Cell Cycle/DNA Damage
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靶点GPR
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受体PFKFB3
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研究领域Cancer
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适应症——
化学信息
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CAS Number1462249-75-7
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分子量328.29
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分子式C18H11F3N2O
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纯度>98% (HPLC)
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溶解度DMSO : ≥ 30 mg/mL; 91.38 mM
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SMILESc12c(ccc(n1)C(F)(F)F)ccc(c2)/C=C/C(=O)c1ccncc1
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化学全称(E)-1-(pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1. Rebecca Redman, et al. Y Res August 1, 2015 75; CT206.
产品手册
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