MS4078

Name: MS4078
Brand: MedChemExpress
SKU: HY-112155
Rating: 5.0 (4 reviews)

Art. -Nr.: HY-112155 Reinheit: 99.72%: Data Sheet
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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.

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MS4078 Chemische Struktur

CAS. Nr. : 2229036-62-6

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10 mM * 1 mL in DMSO ready for reconstitution	Auf Lager	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	Auf Lager	Estimated Time of Arrival: December 31
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10 mg	Auf Lager	Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

4 Publications Citing Use of MCE MS4078

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle PROTACs Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biologische Aktivität
Reinheit & Dokumentation
Verweise
Kundenbewertung

Beschreibung

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^[1].

IC₅₀ & Target

ALK

Cereblon

Cellular Effect

Cell Line	Type	Value	Description	References
NCI-H2228	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
SU-DHL-1	IC₅₀	16 1 Compound: 41; MS4048	Antiproliferative activity against human SU-DHL-1 cells Antiproliferative activity against human SU-DHL-1 cells	[PMID: 35763424]
NCI-H2228	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
SU-DHL-1	IC₅₀	16 1 Compound: 41; MS4048	Antiproliferative activity against human SU-DHL-1 cells Antiproliferative activity against human SU-DHL-1 cells	[PMID: 35763424]
SU-DHL-1	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
NCI-H2228	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human NCI-H2228 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
SU-DHL-1	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]
SU-DHL-1	IC₅₀	33 1 Compound: 6; MS4078	Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay Growth inhibition of human SU-DHL1 cells after 3 days by luminescence-based CellTiter-Glo assay	[PMID: 29627725]

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, 10^0.5 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.

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, 10^0.5 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

Molekulargewicht

914.47

Formel

C₄₅H₅₂ClN₉O₈S

CAS. Nr.

2229036-62-6

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

Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Lösungsmittel & Löslichkeit

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
10 mM	0.1094 mL	0.5468 mL	1.0935 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.

Molaritätsrechner
Verdünnungsrechner

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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.

Reinheit & Dokumentation

Purity: 99.72%

Select Batch:

Data Sheet (274 KB) SDS (394 KB)

COA (246 KB) HNMR (119 KB) RP-HPLC (245 KB) MS (133 KB)

Handling Instructions (2659 KB)

Verweise

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

Complete Stock Solution Preparation Table

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

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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MS4078

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MS4078 Related Antibodies

4 Publications Citing Use of MCE MS4078

Spezialitätsempfehlungen

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Alle PROTACs Isoform-spezifische Produkte anzeigen:

Biologische Aktivität

Reinheit & Dokumentation

Verweise

Kundenbewertung

MS4078 Related Antibodies

Molaritätsrechner

Verdünnungsrechner

Complete Stock Solution Preparation Table

MS4078 Related Classifications

Keywords:

Ihre kürzlich angesehenen Produkte:

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