MS4077 - CAS:2230077-10-6

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MS4077

目录号 : KM8934 CAS No. : 2230077-10-6 纯度 : 98%

Data Sheet 产品使用指南

MS4077 是基于 Cereblon 配体的间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK, K_d 为 37 nM。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

MS4077 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a K_d of 37 nM for binding affinity to ALK.

体外研究

MS4077 effectively inhibits cancer cell proliferation. MS4077 (10-1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC₅₀ of 46 ± 4 nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4077(10-10 μM; 3 days).
MS4077 potently reduces the ALK fusion protein levels and inhibits the ALK auto-phosphorylation and down-steam STAT3 phosphorylation in both SU-DHL-1 and NCI-H2228 cells in a concentration-dependent manner. In SU-DHL-1 cells, MS4077 reduces the NPM-ALK protein levels with impressive DC₅₀ (50% degradation) value of 3±1 nM after 16-hour treatment. Over 90% of inhibition of both ALK Y1507 and STAT3 Y705 phosphorylation is achieved at the 100 nM concentration. In NCI-H2228 cells, MS4077 reduces the EML4-ALK protein levels with similar DC₅₀ value of 34±9 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels.

Cell Viability Assay

Cell Line:	SU-DHL-1 and NCI-H2228 cells
Concentration:	10, 10, 10,10, 10, 10, and 1 μM for SU-DHL-1  cells; 10, 10, 10, 10, 1, 10 μM for NCI-H2228 cells
Incubation Time:	3 days
Result:	Inhibited proliferation of SU-DHL-1 cells (IC₅₀=46 ± 4 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells.

Western Blot Analysis

Cell Line:	SU-DHL-1 and NCI-H2228 cells
Concentration:	1, 3, 10, 30, and 100 μM for SU-DHL-1 cells; 3, 10, 30, 60, and 100 μM for NCI-H2228 cells
Incubation Time:	16 hours
Result:	Reduced the NPM-ALK protein levels with impressive DC₅₀ of  3 ± 1 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC₅₀ of 34 ± 9 nM in NCI-H2228 cells.

分子量

1134.73

CAS号

2230077-10-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 110 mg/mL (96.94 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	0.8813 mL	4.4063 mL	8.8127 mL
5 mM	0.1763 mL	0.8813 mL	1.7625 mL
10 mM	0.0881 mL	0.4406 mL	0.8813 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 (sealed storage, away from moisture and light)。-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 mg/mL (5.29 mM); Suspended solution; Need ultrasonic

此方案可获得 6 mg/mL (5.29 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 60.0 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 6 mg/mL (5.29 mM); Clear solution

此方案可获得 ≥ 6 mg/mL (5.29 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 60.0 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。

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

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