IDF-11774

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Chemical Structure| 1429054-28-3 同义名 : -
CAS号 : 1429054-28-3
货号 : A103226
分子式 : C23H32N2O2
纯度 : 99%+
分子量 : 368.51
MDL号 : MFCD31619285
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Hypoxia-inducible factor (HIF)-1α/β heterodimer binds to the hypoxia-response element (HRE) to induce the transcription of genes related to angiogenesis, metastasis, and resistance in human cancers. IDF-11774 reduced the HRE-luciferase activity of HIF-1α with an IC50 value of 3.65 μM. It also inhibited the accumulation of HIF-1α accumulation under hypoxic conditions in HCT116 human colon cancer cells at the doses of 5-20 μM. Treatment of human umbilical vascular endothelial cells with 20 μM IDF-11774 resulted in a reduction of capillary network formation on Matrigel as compared to DMSO-treated controls. IDF-11774 at 20 μM also decreased the mRNA expression of GLUT1 and pyruvate dehydrogenase kinase, and suppressed the cellular uptake of [3H]2-deoxyglucose in HCT116 cells. Twelve-hour treatment with 10 μM IDF-11774 significantly reduced the levels of intracellular lactate, NAD+ and NADP+. In mice inoculated with HCT116 cells, daily oral administration of IDF-11774 (10, 30, or 60 mg/kg/day) for two weeks significantly inhibited tumor growth at a dose-dependent manner in comparison to vehicle-treated controls[3]. Mechanism: IDF-11774 is a novel HIF-1 inhibitor that suppresses the accumulation of HIF-1α both in vitro and in vivo[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.57mL

2.71mL

1.36mL

27.14mL

5.43mL

2.71mL
参考文献

[1]Ban HS, Kim BK, et al. The novel hypoxia-inducible factor-1α inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumor growth. Cell Death Dis. 2017 Jun 1;8(6):e2843.

[2]Ban HS, Naik R, et al. Identification of Targets of the HIF-1 Inhibitor IDF-11774 Using Alkyne-Conjugated Photoaffinity Probes. Bioconjug Chem. 2016 Aug 17;27(8):1911-20.

[3]Ban HS, Kim BK, Lee H, Kim HM, Harmalkar D, Nam M, Park SK, Lee K, Park JT, Kim I, Lee K, Hwang GS, Won M. The novel hypoxia-inducible factor-1α inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumor growth. Cell Death Dis. 2017 Jun 1;8(6):e2843. doi: 10.1038/cddis.2017.235. PMID: 28569777; PMCID: PMC5520894.