FX-11 LDHA Inhibitor FX11|cas:213971-34-7|西域试剂

FX-11 LDHA Inhibitor FX11,98.44%

产品编号：Bellancom-16214| CAS NO：213971-34-7| 分子式：C₂₂H₂₂O₄| 分子量：350.41

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-16214	￥1900.00	杭州北京（现货）
Bellancom-16214	￥3000.00	杭州北京（现货）
Bellancom-16214	￥14000.00	杭州北京（现货）
Bellancom-16214	￥26000.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

FX-11 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，K_i 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 competitive lactate dehydrogenase A (LDHA) specific inhibitor, with a K_i of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). 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.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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 IC₅₀ values 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.
FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	2.8538 mL	14.2690 mL	28.5380 mL
5 mM	0.5708 mL	2.8538 mL	5.7076 mL
10 mM	0.2854 mL	1.4269 mL	2.8538 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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。