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FX-11
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FX-11图片
CAS NO:213971-34-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
LDHA Inhibitor FX11
产品介绍
FX-11 是一种有效的、选择性的、可逆的和竞争性的乳酸脱氢酶 A (LDHA) 特异性抑制剂,Ki为 8 μM。FX-11 可有效激活PKM2(丙酮酸激酶 M2)。FX-11 降低 ATP 水平,诱导氧化应激、ROS生成和细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植中显示出抗肿瘤 (antitumor) 活性。
生物活性

FX-11 is a potent, selective, reversible and competitivelactate dehydrogenaseA(LDHA) specific inhibitor, with aKiof 8 μM. FX-11 can effectively activatePKM2(pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress,ROSproduction and cell death. FX-11 showsantitumoractivity in lymphoma and pancreaticcancerxenografts[1][2].

IC50& Target

IC50: 23.3 μM (LDHA in HeLa cell)[1].

体外研究
(In Vitro)

FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase[2].
FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells[3].
FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells[2].

Western Blot Analysis[2]

Cell Line:P493 cells
Concentration:9 μM
Incubation Time:24 h, 48 h
Result:Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase.

Cell Proliferation Assay[3]

Cell Line:BxPc-3 and MIA PaCa-2 cells
Concentration:0-100 μM
Incubation Time:72 h
Result:Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC50values of 49.27 μM and 60.54 μM for BxPc-3 and MIA PaCa-2 cells, respectively.
体内研究
(In Vivo)

FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth[2].
FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth[3].

Animal Model:Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)[2]
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)[3]
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.
分子量

350.41

性状

Solid

Formula

C22H22O4

CAS 号

213971-34-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(713.45 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8538 mL14.2690 mL28.5380 mL
5 mM0.5708 mL2.8538 mL5.7076 mL
10 mM0.2854 mL1.4269 mL2.8538 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.94 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.94 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。