NMS-E973 - CAS:1253584-84-7

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NMS-E973

目录号 : KM16112 CAS No. : 1253584-84-7

Data Sheet 产品使用指南

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。

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5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

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.

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.

分子式

C₂₂H₂₂N₄O₇

分子量

454.43

CAS号

1253584-84-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

科研文献

Data Sheet

产品使用指南

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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Other Forms of Rapamycin:

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