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MS-177

Name: MS-177
Brand: TargetMol
SKU: T69771
Rating: 4.5 (1 reviews)

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Catalog No. T69771Cas No. 2225938-86-1

Alias MS177

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.

MS-177

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Catalog No. T69771Alias MS177Cas No. 2225938-86-1

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$81	8-10 weeks	8-10 weeks
5 mg	$197	8-10 weeks	8-10 weeks
10 mg	$313	8-10 weeks	8-10 weeks
25 mg	$619	8-10 weeks	8-10 weeks
50 mg	$993	8-10 weeks	8-10 weeks
100 mg	$1,490	8-10 weeks	8-10 weeks
1 mL x 10 mM (in DMSO)	$397	8-10 weeks	8-10 weeks

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Product Introduction

Bioactivity

Description	MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.MS-177 inhibits the growth of leukemia cells, induces apoptosis, and cell cycle arrest.MS-177 induces degradation of the classical EZH2-PRC2 and the non-classical EZH2-cMyc complexes and activates the immune-responsive genes in MM cells.
Targets&IC50	EOL-1 cells:82% (Dmax), MV-4-11 cells:68% (Dmax), MV-4-11 cells:1.5 µM, EZH2 (PRC2):7 nM, EOL-1 cells:0.2 µM (DC50)
In vitro	MS-177 inhibits the enzymatic activities of EZH2-PRC2 (IC50=7 nM). In EOL-1 and MV4;11 cells, MS-177 exhibited half-maximal degradation concentration (DC50) values of 0.2 µM and 1.5 µM, and maximum degradation (Dmax) values of 82% and 68%. [1]
In vivo	Two doses of MS-177 (100 mg/kg intraperitoneally twice a day, 6 days per week; and 200 mg/kg intraperitoneally twice a day, 3 days per week) were well tolerated in mice and showed no significant toxicity. The antitumor effects of MS-177 were evaluated using a patient-derived xenograft (PDX) animal model of MLL-r AML, and both of the above MS-177 dosing regimens significantly inhibited AML growth in the PDX model, either established by seeding or subcutaneous inoculation, and prolonged survival, relative to controls. [1]
Synonyms	MS177

Chemical Properties

Molecular Weight	914.02
Formula	C₄₈H₅₅N₁₁O₈
Cas No.	2225938-86-1
Smiles	O=C(NCC=1C(=O)NC(=CC1C)C)C2=CC(=CC3=C2C=NN3C(C)C)C=4C=NC(=CC4)N5CCN(CCNC(=O)CCOCCNC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8)CC5

Storage & Solubility Information

Storage

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 120 mg/mL(131.29 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0941 mL	5.4703 mL	10.9407 mL	54.7034 mL
5 mM	0.2188 mL	1.0941 mL	2.1881 mL	10.9407 mL
10 mM	0.1094 mL	0.5470 mL	1.0941 mL	5.4703 mL
20 mM	0.0547 mL	0.2735 mL	0.5470 mL	2.7352 mL
50 mM	0.0219 mL	0.1094 mL	0.2188 mL	1.0941 mL
100 mM	0.0109 mL	0.0547 mL	0.1094 mL	0.5470 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc