EL-102

EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis , inhibits tubulin polymerisation and shows activities against prostate cancer . EL-102 can be used for the research of cancer In Vitro EL-102 (0-120 nM; 72 h) inhibits prostate cancer cells proliferation in vitro. EL-102 (0-100 nM; 72 h) shows cytotoxicity to prostate cancer cell lines. EL-102 (10-100 nM; 24-72 h) induces cellular apoptosis and affects cell cycle. EL-102 (10-100 nM; 24-48 h) affects PARP cleavage in DU145 cells. EL-102 (5 nM; 0-60 min) inhibits tubulin polymerisation activity. EL-102 (0-100 nM; 1 hour) inhibits Hif1α protein expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines Concentration: 0-120 nM Incubation Time: 72 hours Result: Inhibited proliferation of CWR22, 22Rv1, DU145, PC-3, DLKP and doxorubicin-selected variant DLKPA cells with IC 50 s of 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively. Cell Cytotoxicity AssayCell Line: CWR22, 22Rv1, DU145 and PC-3 cell lines Concentration: 0-100 nM Incubation Time: 72 hours Result: Exibited cytotoxicity to prostate cancer cell lines, and showed no additive effect on the inhibition of cell viability with docetaxel. Apoptosis AnalysisCell Line: CWR22, 22Rv1, DU145, PC-3, DLKP and DLKPA cell lines Concentration: 10 and 100 nM Incubation Time: 24, 48 and 72 hours Result: Induced cell apoptosis to inhibits cell viability with a dose of 100 nM. Western Blot AnalysisCell Line: DU145 cell line Concentration: 10 and 100 nM Incubation Time: 24 and 48 hours Result: Increased PARP cleavage in DU145 cells and showed a more dramatic effect with docetaxel adding. Cell Cycle AnalysisCell Line: DU145 cell line Concentration: 10 and 100 nM Incubation Time: 24, 48 and 72 hours Result: Increased loss of cells from G1 phase and accumulated cells in G2/M phase. Western Blot AnalysisCell Line: Prostate cancer cells Concentration: 10 , 50 and 100 nM Incubation Time: 24 and 48 hours Result: Modestly inhibited Hif1α expression at doses of 50 and 100 nM in normoxia. In Vivo EL-102 (12 and 15 mg/kg; p.o. 5-day on and 2-day off, from 13 to 37 days after tumour transplantation) potentiates effects of docetaxel in vivo . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice with CWR22 xenografts Dosage: 12 and 15 mg/kg Administration: Oral gavage; 12 and 15 mg/kg 5-day on and 2-day off; from 13 to 37 days after tumour transplantation Result: Showed no effect on tumor growth, but enhanced the effect of docetaxel on tumor . Form:Solid IC50& Target:IC50: 24 nM (CWR22), 21.7 nM (22Rv1), 40.3 nM (DU145), 37.0 nM (PC-3), 14.4 nM (DLKP), 16.3 nM (DLKPA)

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