MS4078 - CAS:2229036-62-6

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MS4078

目录号 : KM7359 CAS No. : 2229036-62-6 纯度 : 98%

Data Sheet 产品使用指南

MS4078 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 19 nM。

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5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

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

体外研究

MS4078 effectively inhibits cancer cell proliferation. MS4078 (10, 10, 10, 10, 10, 10, 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, 10, 10, 10, 1, 10 μM; 3 days).
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.

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=33 ± 1 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  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

分子式

C₄₅H₅₂ClN₉O₈S

分子量

914.47

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。

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

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