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MS4078
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
MS4078图片
CAS NO:2229036-62-6
包装与价格：
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

MS4078 is ananaplastic lymphoma kinase(ALK)PROTAC(degrader) based onCereblonligand, with aKdof 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, 100.5μM; 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 DC50value 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].

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, 100.5μM 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 DC50of 11 ± 2 nM in SU-DHL-1 cells. Reduced the EML4-ALK protein levels with similar DC50of 59 ± 16 nM in NCI-H2228 cells
分子量

914.47

性状

Solid

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°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 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 mg5 mg10 mg
1 mM1.0935 mL5.4676 mL10.9353 mL
5 mM0.2187 mL1.0935 mL2.1871 mL
10 mM0.1094 mL0.5468 mL1.0935 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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本网站选购。