NMS-E973|cas:1253584-84-7|西域试剂

NMS-E973,98.57%

产品编号：Bellancom-17547| CAS NO：1253584-84-7| 分子式：C₂₂H₂₂N₄O₇| 分子量：454.43

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货号	价格	库存与货期
Bellancom-17547	￥900.00	杭州北京（现货）
Bellancom-17547	￥1500.00	杭州北京（现货）
Bellancom-17547	￥3200.00	杭州北京（现货）
Bellancom-17547	￥5200.00	杭州北京（现货）
Bellancom-17547	￥8400.00	杭州北京（现货）

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NMS-E973

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (110.03 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2006 mL	11.0028 mL	22.0056 mL
5 mM	0.4401 mL	2.2006 mL	4.4011 mL
10 mM	0.2201 mL	1.1003 mL	2.2006 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.50 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.50 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (5.50 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.50 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明