MS4078

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MS4078  纯度: 99.63%

MS4078 是基于 Cereblon 配体的间变性淋巴瘤激酶 (ALK) PROTAC (降解物)，结合 ALK，Kd 为 19 nM。

MS4078

MS4078 Chemical Structure

CAS No. : 2229036-62-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2010 In-stock
5 mg ￥1300 In-stock
10 mg ￥2000 In-stock
50 mg ￥5600 In-stock
100 mg ￥9000 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

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生物活性

MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK[1].

IC50 & Target

ALK

 

Cereblon

 

体外研究
(In Vitro)

MS4078 effectively inhibits cancer cell proliferation. MS4078 (10-3, 10-2.5, 10-2, 10-1.5, 10-1, 10-0.5, 1 μM; 3 days) concentration-dependently inhibits proliferation of SU-DHL-1 cells with an IC50 of 33±1  nM. In comparison with SU-DHL-1 cells, the proliferation of NCI-H2228 cells is less sensitive to MS4078(10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM; 3 days)[1].
MS4078 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, MS4078 reduces the NPM-ALK protein levels with impressive DC50 (50% degradation) value of 11±2 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, MS4078 reduces the EML4-ALK protein levels with similar DC50 value of 59 ± 16 nM after 16-hour treatment. At the 100 nM concentration, NCI-H2228 cells reduces more than 90% of EML4-ALK protein levels[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SU-DHL-1 and NCI-H2228 cells
Concentration: 10-3, 10-2.5, 10-2,10-1.5, 10-1, 10-0.5, and 1 μM for SU-DHL-1  cells; 10-2, 10-1.5, 10-1, 10-0.5, 1, 100.5 μM for NCI-H2228 cells
Incubation Time: 3 days
Result: Inhibited proliferation of SU-DHL-1 cells (IC50=33 ± 1 nM). Less sensitive to the proliferation of NCI-H2228 cells than SU-DHL-1 cells.

Western Blot Analysis[1]

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  11 ± 2 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC50 of 59 ± 16 nM in NCI-H2228 cells

分子量

914.47

Formula

C45H52ClN9O8S
CAS 号

2229036-62-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL (54.68 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.0935 mL 5.4676 mL 10.9353 mL
5 mM 0.2187 mL 1.0935 mL 2.1871 mL
10 mM 0.1094 mL 0.5468 mL 1.0935 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    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (2.27 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.08 mg/mL (2.27 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 20.8 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
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Zhang C, et al. Proteolysis Targeting Chimeras (PROTACs) of Anaplastic Lymphoma Kinase (ALK). Eur J Med Chem. 2018 May 10;151:304-314.

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