Art. -Nr.: HY-162250

MS8847

Name: MS8847
Brand: MedChemExpress
SKU: HY-162250
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MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer.
(Pink: EZH2 ligand (HY-185582); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

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Reinheit : 99.78%
CAS. Nr.: 3050872-59-5
Formel: C₇₀H₉₈N₁₀O₈S
Molecular Weight:1239.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MS8847 Chemical Structure

CAS. Nr.: 3050872-59-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Protokoll (2)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer^[1]. (Pink: EZH2 ligand (HY-185582); Blue: VHL ligand (HY-125845); Black: linker (HY-W014831)).

IC₅₀ & Target

VHL

EZH2

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BT-549	IC₅₀	1.45 μM Compound: 8; MS8847	Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human BT-549 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
EOL1	IC₅₀	0.11 μM Compound: 8; MS8847	Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human EOL1 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
MDA-MB-468	IC₅₀	0.45 μM Compound: 8; MS8847	Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
MV4-11	IC₅₀	0.17 μM Compound: 8; MS8847	Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human MV4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]
RS4-11	IC₅₀	0.41 μM Compound: 8; MS8847	Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay Anti-proliferative activity against human RS4-11 cells assessed as cell viability measured after 5 days incubation by CCK-8 assay	[PMID: 38295690]

In Vitro

MS8847 selectively targets EZH2-dependent cell growth and inhibits the proliferation of triple-negative breast cancer (TNBC) cells, with 5-day IC₅₀ values of 1.45 μM (BT549) and 0.45 μM (MDA-MB-468), respectively. It also inhibits the proliferation of MLL-r AML cell lines, with 5-day IC₅₀ values of 0.11 μM (EOL-1), 0.17 μM (MV4;11) and 0.41 μM (RS4;11), respectively^[1].
MS8847 (0.1-1 μM; 24 h) completely degrades EZH2 protein in EOL-1 MLL-r AML cells^[1].
MS8847 (1 nM-0.3 μM; 24 h) potently degrades EZH2 in a concentration-dependent manner in EOL-1 MLL-rAML cells, with a DC₅₀ of 34.4 nM, and also degrades EED and SUZ12^[1].
MS8847 (2.5-20 μM; 5 d) significantly inhibits cell growth and reduces spheroid size in a 3D in vitro BT549 TNBC model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

Western Blot Analysis^[1]

View Protocol

Cell Line:

EOL-1 (MLL-r AML cell line)
Concentration:

1-1000 nM; 0.03-0.3 μM
Incubation Time:

24 h
Result:

Achieved a half-maximal degradation concentration (DC₅₀) of 34.4 nM for EZH2.
Potently degraded PRC2 core component EED, and degraded SUZ12 to a lesser extent.
Reduced the H3K27me3 mark.

Western Blot Analysis^[1]

View Protocol

Cell Line:

EOL-1 (MLL-r AML cell line)
Concentration:

300 nM
Incubation Time:

2 h; 4 h; 8 h; 12 h; 24 h; 48 h
Result:

Initiated EZH2 degradation at 8 h and reached maximum degradation by 24 h.
Reduced the H3K27me3 mark over time.

Western Blot Analysis^[1]

View Protocol

Cell Line:

EOL-1 (MLL-r AML cell line)
Concentration:

0.03-0.3 μM (direct treatment); 0.5 μM (post 2 h pre-incubation with inhibitors/ligands)
Incubation Time:

24 h (direct treatment); 24 h (post 2 h pre-incubation with inhibitors/ligands)
Result:

Effectively induced EZH2 degradation at 0.03, 0.1, 0.3 μM.
Rescued EZH2 degradation induction via pre-treatment with MLN4942, EPZ-6438, or VHL-1.
Failed to induce EZH2 degradation with negative controls MS8847N1 and MS8847N2.

Western Blot Analysis^[1]

View Protocol

Cell Line:

EOL-1, MV4;11, RS4;11 (MLL-r AML cell lines)
Concentration:

0.03-0.3 μM
Incubation Time:

24 h
Result:

Induced complete EZH2 degradation at 0.1 and 0.3 μM in EOL-1 cells.
Induced near-complete EZH2 degradation at 0.03, 0.1, 0.3 μM in MV4;11 cells.
Induced EZH2 degradation at 0.1 and 0.3 μM in RS4;11 cells.

Western Blot Analysis^[1]

View Protocol

Cell Line:

BT549, MDA-MB-468 (TNBC cell lines)
Concentration:

0.1-3 μM
Incubation Time:

48 h
Result:

Induced potent EZH2 degradation in both BT549 and MDA-MB-468 cells following 48 h treatment.

Parmacokinetics

Species	Dose	Route	C_max	Plasma Concentration
Mice^[1]	50 mg/kg	i.p.	3.9 μM	>1 μM

In Vivo

MS8847 (50 mg/kg; i.p.; single dose) achieves sustained plasma concentrations in male Swiss Albino mice and is well tolerated following a single 50 mg/kg intraperitoneal injection^[1].

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

Animal Model:

Swiss Albino (male)^[1]
Dosage:

50 mg/kg
Administration:

i.p.; single dose
Result:

Observed a maximum plasma concentration (C_max) of 3.9 μM at 4 hours.
Retained over 1 μM in plasma at 9 hours.
Exhibited no obvious clinical signs of toxicity at the tested dose.

Chemical Information

CAS. Nr. 3050872-59-5
Appearance Solid
Molecular Weight 1239.65
Formel C₇₀H₉₈N₁₀O₈S
Color White to off-white
SMILES

CC1=CC(C)=C(CNC(C2=C(C)C(N(C3CCOCC3)CC)=CC(C4=CC=C(CN5CCN(CCC(NCCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N6[C@H](C(NCC7=CC=C(C8=C(C)N=CS8)C=C7)=O)C[C@@H](O)C6)=O)=O)=O)CC5)C=C4)=C2)=O)C(N1)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (80.67 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

0.8067 mL

4.0334 mL

8.0668 mL

5 mM

0.1613 mL

0.8067 mL

1.6134 mL

10 mM

0.0807 mL

0.4033 mL

0.8067 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Protokoll

All Animals and Diseases Cell Biology

Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Velez J, et al. Discovery of a novel, highly potent EZH2 PROTAC degrader for targeting non-canonical oncogenic functions of EZH2. Eur J Med Chem. 2024;267:116154. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	0.8067 mL	4.0334 mL	8.0668 mL	20.1670 mL
	5 mM	0.1613 mL	0.8067 mL	1.6134 mL	4.0334 mL
	10 mM	0.0807 mL	0.4033 mL	0.8067 mL	2.0167 mL
	15 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3445 mL
	20 mM	0.0403 mL	0.2017 mL	0.4033 mL	1.0083 mL
	25 mM	0.0323 mL	0.1613 mL	0.3227 mL	0.8067 mL
	30 mM	0.0269 mL	0.1344 mL	0.2689 mL	0.6722 mL
	40 mM	0.0202 mL	0.1008 mL	0.2017 mL	0.5042 mL
	50 mM	0.0161 mL	0.0807 mL	0.1613 mL	0.4033 mL
	60 mM	0.0134 mL	0.0672 mL	0.1344 mL	0.3361 mL
	80 mM	0.0101 mL	0.0504 mL	0.1008 mL	0.2521 mL

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MS8847

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen