货号	规格	价格	上海	北京	珠海	重庆	武汉
S82501-1mg	≥99%	￥740.00 S82501-1mg ￥740.00 3-5天	0 货期：3-5天	-	-	-	-
S82501-5mg	≥99%	￥1980.00 S82501-5mg ￥1980.00 3-5天	0 货期：3-5天	-	-	-	-
S82501-10mg	≥99%	￥3130.00 S82501-10mg ￥3130.00 3-5天	0 货期：3-5天	-	-	-	-
S82501-50mg	≥99%	￥6880.00 S82501-50mg ￥6880.00 3-5天	0 货期：3-5天	-	-	-	-
S82501-100mg	≥99%	￥9270.00 S82501-100mg ￥9270.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

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

靶点：

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);MicrotubuleAssociated; HIF

体外研究：

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 hours Result: 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 cel

体内研究：

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 .

参考文献：

1. A P Toner et al. The novel toluidine sulphonamide EL102 shows pre-clinical in vitro and in vivoactivity against prostate cancer and circumvents MDR1 resistance. Br J Cancer, 2013 Oct 15, 109(8): 2131-2141.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.601 ml	13.005 ml	26.01 ml
5 mM	0.52 ml	2.601 ml	5.202 ml
10 mM	0.26 ml	1.3 ml	2.601 ml
50 mM	0.052 ml	0.26 ml	0.52 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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