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IDF-11774

カタログ番号GC32948

IDF-11774 は、IC50 が 3.65 μM の新しい低酸素誘導因子 α (HIFα)-1 阻害剤です。

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IDF-11774 化学構造

Cas No.: 1429054-28-3

サイズ 価格 在庫数 個数
10mM (in 1mL DMSO)
$70.00
在庫あり
1mg
$50.00
在庫あり
5mg
$87.00
在庫あり
10mg
$137.00
在庫あり
50mg
$570.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of IDF-11774

IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC50 of 3.65 μM. IDF-11774 has been approved as a clinical candidate for a phase I study.

IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC50 of 3.65 μM in cancer cell line. IDF-11774 has been approved as a clinical candidate for a phase I study. Human umbilical vascular endothelial cells (HUVECs) treated with IDF-11774 show reduced capillary network formation on Matrigel. IDF-11774 treatment leads to reduced mRNA expression of GLUT1 and pyruvate dehydrogenase kinase 1 (PDK1). In addition, intracellular ATP levels are significantly reduced in the presence of IDF-11774 and are affected to a greater degree under low glucose conditions (5.5 mM)[1].

Luciferase activity and HIF-1α accumulation are strongly suppressed in the tumors of mice treated by oral administration of IDF-11774, compare with the control. When IDF-11774 is orally administered daily for two weeks, significant dose-dependent tumor regression is observed in the mouse model[1].

[1]. Ban HS, 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.

Protocol of IDF-11774

Animal experiment:

Female Balb/c nude mice are used in this study. Cancer cells are injected subcutaneously into 4- to 6-week-old female Balb/c nude mice to generate tumors (5 mice per group). When the tumors grow to 100 mm3, IDF-11774 is administered orally (per oral) or intravenously for 15 days. Tumor volumes (V) are determined using the following equation: V (mm3)=(length×width×height)×0.5. Percentage tumor growth inhibition (%TGI) values are calculated for each treatment group versus the control[1].

References:

[1]. Ban HS, 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.

Chemical Properties of IDF-11774

Cas No. 1429054-28-3 SDF
Canonical SMILES CN1CCN(C(COC2=CC=C(C3(C4)CC5CC4CC(C5)C3)C=C2)=O)CC1
Formula C23H32N2O2 M.Wt 368.51
溶解度 DMSO : 60 mg/mL (162.82 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of IDF-11774

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1 mg 5 mg 10 mg
1 mM 2.7136 mL 13.5682 mL 27.1363 mL
5 mM 0.5427 mL 2.7136 mL 5.4273 mL
10 mM 0.2714 mL 1.3568 mL 2.7136 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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