MS1943|MS1943|cas:2225938-17-8|西域试剂

MS1943,MS1943,99%

产品编号：Bellancom-133129| CAS NO：2225938-17-8| 分子式：C₄₂H₅₄N₈O₃| 分子量：718.93

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货号	价格	库存与货期
Bellancom-133129	￥480.00	杭州北京（现货）
Bellancom-133129	￥850.00	杭州北京（现货）
Bellancom-133129	￥1500.00	杭州北京（现货）
Bellancom-133129	￥2900.00	杭州北京（现货）
Bellancom-133129	￥5100.00	杭州北京（现货）
Bellancom-133129	￥8500.00	杭州北京（现货）

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MS1943

产品介绍

MS1943 是一种首创的，具有口服生物活性的 EZH2 选择性降解剂，其 IC₅₀ 为 120 nM。MS1943 显著降低了许多三阴性乳腺癌和其他癌及非癌细胞系中的EZH2蛋白水平。MS1943 有效地阻止了多个三阴性乳腺癌和其他癌细胞系的增殖。

生物活性

MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC₅₀ of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.

体外研究

MS1943 (0.625-5 μM; 3 days) inhibits cell growth with an GI₅₀ of 2.2 µM.
MS1943 (0.625-5 μM; 4 days) induces cell death in MDA-MB-468 cells. MS1943 effectively reduces EZH2 levels in BT549, HCC70 and MDA-MB-231 TNBC cells, as well as KARPAS-422 and SUDHL8 lymphoma cells and PNT2 non-cancerous prostate cells.
MS1943 (1.25-5.0 μM; 2 days) inhibits EZH2 and SUZ12 protein levels in a concentration- and timedependent manner, without affecting EED protein levels, whereas the H3K27me3 mark was also suppressed.

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

Cell Viability Assay

Cell Line:	MDA-MB-468 cells
Concentration:	0.625, 1.25, 2.5, 5 μM
Incubation Time:	3 days
Result:	Inhibits cell growth with an GI₅₀ of 2.2 µM.

Western Blot Analysis

Cell Line:	MDA-MB-468 cells
Concentration:	1.25, 2.5, 5.0 μM
Incubation Time:	2 days
Result:	Reduced EZH2 protein levels in a concentration- and time-dependent manner.

体内研究
(In Vivo)

MS1943 (150 mg/kg body weight; i.p.; once daily for 36 days) suppresses tumor growth.
MS1943 induces apoptosis in the MDA-MB-468 xenograft model.
A single i.p. injection of MS1943 at 50 mg/kg body weight achieved a peak plasma concentration (Cmax) of 2.9 µM and resulted in plasma concentrations above its cellular IC₅₀ value for ~2h. A single 150 mg/kg body weight p.o. dose achieved Cmax of 1.1 µM, but plasma concentrations were below the cellular IC₅₀ value.

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

Animal Model:	Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)
Dosage:	150 mg/kg body weight
Administration:	i.p.; once daily for 36 days
Result:	Suppresses tumor growth.

体内研究

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

Animal Model:	Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)
Dosage:	150 mg/kg body weight
Administration:	i.p.; once daily for 36 days
Result:	Suppresses tumor growth.

体内研究

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

Animal Model:	Eight-week-old female BALB/c nude mice (MDA-MB-468 xenografts)
Dosage:	150 mg/kg body weight
Administration:	i.p.; once daily for 36 days
Result:	Suppresses tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (173.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.3910 mL	6.9548 mL	13.9096 mL
5 mM	0.2782 mL	1.3910 mL	2.7819 mL
10 mM	0.1391 mL	0.6955 mL	1.3910 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: ≥ 6.25 mg/mL (8.69 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (8.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 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: ≥ 6.25 mg/mL (8.69 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (8.69 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 62.5 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 6.25 mg/mL (8.69 mM); Clear solution

此方案可获得 ≥ 6.25 mg/mL (8.69 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 62.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。