产品
编 号:F272723
分子式:C22H22O4
分子量:350.41
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10mM*1mL in DMSO
1672
In-stock
5mg
1520
In-stock
10mg
2400
In-stock
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生物活性:
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts.

体内研究:
FX-11 (42 μg/小鼠;IP,每日一次,持续 10-14 天) 抑制 P493 肿瘤生长。FX-11 (0-2 mg/kg,IP,每天,持续 3 周) 显著延缓肿瘤生长。Animal Model:Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)
Dosage:42 μg/mouse (2.1 mg/kg)
Administration:IP; daily for 10-14 days
Result:Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression.
Animal Model:Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)
Dosage:2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46
Administration:IP (100 μL), daily, for 3 weeks
Result:Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth.

体外研究:
FX-11 (9 μM,24-48 h) 显示 AMP 激酶的激活及其底物乙酰辅酶 A 羧化酶的磷酸化。FX-11 在 P493 细胞中抑制糖酵解并改变细胞能量代谢。FX-11 (0-100 μM,72 h) 在 BxPc-3 和 MIA PaCa-2 细胞中抑制细胞增殖。
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