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NMS-E973
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NMS-E973图片
CAS NO:1253584-84-7
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
NMS-E973 是一种有效的,可透过血脑屏障的选择性HSP90抑制剂。NMS-E973 与Hsp90α的 ATP 位点结合,DC50小于 10 nM。NMS-E973 能够穿越血脑屏障 (BBB)。具有抗肿瘤效果。
生物活性

NMS-E973 is a potent and selective inhibitor ofHSP90. NMS-E973 binds to the ATP binding site ofHsp90αwith aDC50of<10 nm. nms-e973 is able to cross the blood-brain barrier (bbb). antitumor efficacy[1].

IC50& Target[1]

HSP90α

10 nM (DC50)

体外研究
(In Vitro)

NMS-E973 inhibits cancer cell proliferation. NMS-E973 shows a widespread antiproliferative activity, with an average IC50of 1.6 μM and 15 cell lines with an IC50<100 nm[1].

Cell Proliferation Assay[1]

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 IC50of 133 nM for A-375 cell.
体内研究
(In Vivo)

NMS-E973 (60 mg/kg; i.v.) inhibits the growth of A375 tumors subcutaneously or intracranially implanted in mice[1].
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[1].

Animal Model:Balb/c male nude mice (aged 6 to 8 weeks) xenografted with the A375 tumors[1]
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.
分子量

454.43

性状

Solid

Formula

C22H22N4O7

CAS 号

1253584-84-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month