IDF-11774-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIDF-11774Cat. No.: HY-111387CAS No.: 1429054-28-3分式: CHNO分量: 368.51作靶點(diǎn): HIF/HIF Prolyl-Hydroxylase作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 60 mg/mL (162

2、.82 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.7136 mL 13.5682 mL 27.1363 mL5 mM 0.5427 mL 2.7136 mL 5.4273 mL10 mM 0.2714 mL 1.3568 mL 2.7136 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液

3、，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.67 mg/mL (4.53 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1.67 mg/mL (4.53 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolub

4、ility: 1.67 mg/mL (4.53 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 IDF-11774種新型低氧誘導(dǎo)因 (HIF)-1 的抑制劑，其 IC50 值為 3.65 M。IC50 & Target IC50: 3.65 M (HIF-1) 1體外研究 IDF-11774 is a novel hypoxia-inducible factor (HIF)-1 inhibitor with an IC50 of 3.65 M in cancer

5、 cell line.IDF-11774 has been approved as a clinical candidate for a phase I study. Human umbilical vascularendothelial 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

6、kinase 1(PDK1). In addition, intracellular ATP levels are significantly reduced in the presence of IDF-11774 and areaffected to a greater degree under low glucose conditions (5.5mM) 1.體內(nèi)研究 Luciferase activity and HIF-1 accumulation are strongly suppressed in the tumors of mice treated by oraladminis

7、tration of IDF-11774, compare with the control. When IDF-11774 is orally administered daily for twoweeks, significant dose-dependent tumor regression is observed in the mouse model 1.PROTOCOLAnimal Female Balb/c nude mice are used in this study. Cancer cells are injected subcutaneously into 4- to 6-

8、week-Administration 1 old female Balb/c nude mice to generate tumors (5 mice per group). When the tumors grow to 100mm3, IDF-11774 is administered orally (per oral) or intravenously for 15 days. Tumor volumes (V) are determined usingthe following equation: V (mm3)=(lengthwidthheight)0.5. Percentage

9、tumor growth inhibition (%TGI)values are calculated for each treatment group versus the control 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Ban HS, et al. The novel hypoxia-inducible factor-1 inhibitor IDF-11774 regulates cancer metabolism, thereby suppressing tumorgrowth. Cell Death Dis. 2017 Jun 1;8(6):e2843.McePdfHeightCaution: Product has not been fully validated for m