FX-11

(Synonyms: LDHA Inhibitor FX11)
目录号: PL10935 纯度: ≥98%
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。
CAS No. :213971-34-7
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中文名称
FX-11
英文名称
FX-11
英文别名
2,3-Dihydroxy-6-methyl-7-(phenylmethyl)-4-propyl-1-naphthalenecarboxylic Acid;7-Benzyl-2,3-dihydroxy-6-methyl-4-propyl-1-naphthoic acid;FX-11;LDHA Inhibitor FX11;FX11;7-benzyl-2,3-dihydroxy-6-methyl-4-propylnaphthalene-1-carboxylic acid;7-benzyl-2,3-dihydroxy-6-methyl-4-propyl-naphthalene-1-carboxylic Acid;LDHA Inhibitor, 3;FX 11;BDBM50066974;3-dihydroxy-6-methyl-7-(phenylmethyl)-4-propylnaphthalene-1-carboxylic acid;2,3-Dihydroxy-4-propyl-6-methyl-7-benzylnaphthalene-1-carboxyl
Cas No.
213971-34-7
分子式
C22H22O4
分子量
350.41
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
详情描述
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。
产品详情
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 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.
性状
Solid
IC50 & Target[1][2]
IC50: 23.3 μM (LDHA in HeLa cell) .
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.
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. has not independently confirmed the accuracy of these methods. They are for reference only.Western Blot Analysis
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. EC Calvaresi. Small molecule inhibitors of lactate dehydrogenase a as an anticancer strategy. 2014.
[2]. Le A, et, al. Inhibition of lactate dehydrogenase A induces oxidative stress and inhibits tumor progression. Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2037-42.
[3]. Mohammad GH, et al. Targeting Pyruvate Kinase M2 and Lactate Dehydrogenase A Is an
溶解度数据
In Vitro: DMSO : 250 mg/mL (713.45 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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