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• 产品描述： PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria

• 靶点： IC50 : 137 nM (PFKFB3);Apoptosis; Glucokinase; Autophagy

• 体外研究：
  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.

• 体内研究：
  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.

• 参考文献：
  1. Mondal S, et al. Therapeutic targeting of PFKFB3 with a novel glycolytic inhibitor PFK158 promotes lipophagy and chemosensitivity in gynecologic cancers. Int J Cancer. 2019 Jan 1;144(1):178-189. 2. Zhang Y, et al. Synergistic Effect of Colistin Combined with PFK-158 against Colistin-Resistant Enterobacteriaceae. Antimicrob Agents Chemother. 2019 Jun 24;63(7). pii: e00271-19. 3. Pooran Chand, et al. Pfkfb3 inhibitor and methods of use as an anti-cancer therapeutic. WO2013148228A1.

• 溶解性： soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	3.046 ml	15.231 ml	30.461 ml
  5 mM	0.609 ml	3.046 ml	6.092 ml
  10 mM	0.305 ml	1.523 ml	3.046 ml
  50 mM	0.061 ml	0.305 ml	0.609 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *