货号	规格	价格	上海	北京	珠海	重庆	武汉
S89712-5mg买3赠1	99.60%	￥440.00 S89712-5mg ￥440.00 现货（买3赠1）	6 6	-	-	-	-
S89712-10mg买3赠1	99.60%	￥730.00 S89712-10mg ￥730.00 现货（买3赠1）	7 7	-	-	-	-
S89712-25mg买3赠1	99.60%	￥1550.00 S89712-25mg ￥1550.00 现货（买3赠1）	4 4	-	-	-	-
S89712-100mg	≥98%	￥3250.00 S89712-100mg ￥3250.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy

靶点：

HSP90α:10 nM (DC50);HSP

体外研究：

NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50 of 1.6 μM and 15 cell lines with an IC50 <100 nM. Cell Proliferation Assay Cell Line: Carcinoma breast DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells; Leukemia MV-4-11 and MOLM-13 cells; Melanoma A-375 cells Concentration: Incubation Time: 24, 48, 72 hours Result: IC50s of 13, 16, 56, 61, 73, 76, and 89 nM for DU-4475, EVSA-T, CAL-51, HCC1954, BT-474, HCC1419, HDQ-P1 cells, respectively.IC50s of 29 and 35 nM for MV-4-11, MOLM-13 cells, respectively.The IC50 of 133 nM for A-375 cell.

体内研究：

NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice. NMS-E973 exhibits moderate elimination half-lives (5.55±1.07 h) due to high plasma clearance (39.9±1.70 mL/min/kg) combined with large volumes of distribution (5.83±3.18 L/kg) following intravenous administration (10 mg/kg) in mice. Animal Model: Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors Dosage: 60 mg/kg Administration: Administered twice daily i.v. according to 2 schedules: (i) every other day for 12 days and (ii) 3 days on/1 day off/3 days on (3-1-3, one cycle). Result: Both schedules resulted in tumor shrinkage and TGI of 74% and 89%, respectively.

参考文献：

1. Gianpaolo Fogliatto, et al. NMS-E973, a novel synthetic inhibitor of Hsp90 with activity against multiple models of drug resistance to targeted agents, including intracranial metastases. Clin Cancer Res. 2013 Jul 1;19(13):3520-32.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.201 ml	11.003 ml	22.006 ml
5 mM	0.44 ml	2.201 ml	4.401 ml
10 mM	0.22 ml	1.1 ml	2.201 ml
50 mM	0.044 ml	0.22 ml	0.44 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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