EL-102

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

EL-102 是 hypoxia-induced factor 1 (Hif1α) 的抑制剂。EL-102 诱导细胞凋亡，抑制微管蛋白聚合，并显示抗前列腺癌活性。EL-102 可用于癌症的研究。

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.

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.Cell Proliferation Assay Cell 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 IC50s of 24, 21.7, 40.3, 37.0, 14.4 and 16.3 nM, respectively.Cell Cytotoxicity Assay Cell Line:CWR22, 22Rv1, DU145 and PC-3 cell lines Concentration:0-100 nM Incubation Time:72 hoursResult:Exibited cytotoxicity to prostate cancer cell lines, and showed no additive effect on the inhibition of cell viability with docetaxel.Apoptosis Analysis Cell 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 Analysis Cell 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 Analysis Cell 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 Analysis Cell 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.

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.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 .

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Others

Other Targets

Microtubule Associated | HIF

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1233948-61-2

384.47

C19H16N2O3S2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : ≥ 36 mg/mL (93.64 mM)

COc1ccc(cc1)S(=O)(=O)Nc1cc(ccc1C)-c1csc(c1)C#N

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(-20℃)

With Ice Pack

≥ 2 years