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CAS No.: 1429054-28-3

IDF-11774 Catalog No. CSN20256

Synonyms: IDF-11774

IDF-11774 is a hypoxia-inducible factor (HIF)-1α inhibitor which regulates cancer metabolism, thereby suppressing tumor growth.

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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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.7136 mL
- 13.5681 mL
- 27.1361 mL
- 5 mM
- 0.5427 mL
- 2.7136 mL
- 5.4272 mL
- 10 mM
- 0.2714 mL
- 1.3568 mL
- 2.7136 mL

技术信息

CAS号

1429054-28-3

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H32N2O2

运输

蓝冰

分子量

368.51

别名

IDF-11774

溶解度

DMSO	20.71 mg/mL (56.2 mM)
Water	insoluble

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