货号	规格	价格	上海	北京	珠海	重庆	武汉
S83421-5mg买3赠1	99.90%	￥600.00 S83421-5mg ￥600.00 现货（买3赠1）	4 4	-	-	-	-
S83421-10mg买3赠1	99.90%	￥920.00 S83421-10mg ￥920.00 现货（买3赠1）	6 6	-	-	-	-
S83421-25mg买3赠1	99.90%	￥1690.00 S83421-25mg ￥1690.00 现货（买3赠1）	5 5	-	-	-	-
S83421-50mg买3赠1	99.90%	￥2620.00 S83421-50mg ￥2620.00 现货（买3赠1）	5 5	-	-	-	-
S83421-100mg买3赠1	99.90%	￥4100.00 S83421-100mg ￥4100.00 现货（买3赠1）	4 4	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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