2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Anaplastic lymphoma kinase (ALK)
  4. MS4078

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

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MS4078 Chemical Structure

MS4078 Chemical Structure

CAS No. : 2229036-62-6

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10 mM * 1 mL in DMSO
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Customer Review

Based on 1 publication(s) in Google Scholar

MS4078 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MS4078

View All PROTACs Isoform Specific Products:

View All Isoforms
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MS4078 Related Antibodies

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
Molecular Weight

914.47

Formula

C45H52ClN9O8S
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC(C)S(C1=C(NC2=NC(NC3=C(OC(C)C)C=C(C4CCN(CC(NCCNC5=C(C(N(C6C(NC(CC6)=O)=O)C7=O)=O)C7=CC=C5)=O)CC4)C(C)=C3)=NC=C2Cl)C=CC=C1)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (54.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.63%

COA (246 KB) HNMR (209 KB) LCMS (110 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.0935 mL 5.4676 mL 10.9353 mL 27.3382 mL
5 mM 0.2187 mL 1.0935 mL 2.1871 mL 5.4676 mL
10 mM 0.1094 mL 0.5468 mL 1.0935 mL 2.7338 mL
15 mM 0.0729 mL 0.3645 mL 0.7290 mL 1.8225 mL
20 mM 0.0547 mL 0.2734 mL 0.5468 mL 1.3669 mL
25 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0935 mL
30 mM 0.0365 mL 0.1823 mL 0.3645 mL 0.9113 mL
40 mM 0.0273 mL 0.1367 mL 0.2734 mL 0.6835 mL
50 mM 0.0219 mL 0.1094 mL 0.2187 mL 0.5468 mL
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MS4078 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MS40782229036-62-6MS 4078MS-4078PROTACsAnaplastic lymphoma kinase (ALK)Anaplastic lymphoma kinaseALK tyrosine kinase receptorCD246Cluster of differentiation 246Inhibitorinhibitorinhibit

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