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Referencia número: HY-189760

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S-023-0996

S-023-0996 is an orally active EZH2/EGFR dual-target inhibitor. S-023-0996 inhibits EZH2 catalytic function and EGFR kinase activity, with IC₅₀ values of 2.41 nM and 42.18 nM, respectively. S-023-0996 exhibits selective cytotoxicity against tumor cells and inhibits TNBC cell migration and invasion. S-023-0996 inhibits TNBC primary tumor growth and metastasis in vivo. S-023-0996 can be used for research on triple-negative breast cancer (TNBC).

Para uso exclusivo en investigación. No vendemos a pacientes.

Fòrmula: C₄₉H₆₀N₈O₆
Peso molecular:857.05

Almacenamiento:

Please store the product under the recommended conditions in the Certificate of Analysis.

S-023-0996 Chemical Structure

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Use of MCE Products

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Pureza y Documentación
Referencias
Calculators
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Classifications
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Actividad biológica

Descripciòn

IC₅₀ & Target

^[1]

EGFR

42.18 nM (IC₅₀)

EZH2

2.41 nM (IC₅₀)

Ver todos los productos específicos de isoformas Histone Methyltransferase :

Ver todos los productos específicos de isoformas EGFR :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1806	IC50	8.45 μM	Antiproliferative activity against human HCC1806 TNBC cells assessed by SRB assay. Antiproliferative activity against human HCC1806 TNBC cells assessed by SRB assay.	42642931
MDA-MB-231	IC50	6.19 μM	Antiproliferative activity against human MDA-MB-231 TNBC cells assessed by SRB assay. Antiproliferative activity against human MDA-MB-231 TNBC cells assessed by SRB assay.	42642931
MDA-MB-468	IC50	4.25 μM	Antiproliferative activity against human MDA-MB-468 TNBC cells assessed by SRB assay. Antiproliferative activity against human MDA-MB-468 TNBC cells assessed by SRB assay.	42642931
4T1	IC50	6.99 μM	Antiproliferative activity against murine 4T-1 TNBC cells assessed by SRB assay. Antiproliferative activity against murine 4T-1 TNBC cells assessed by SRB assay.	42642931
Vero	IC50	>100 μM	Antiproliferative activity against african green monkey Vero cells assessed by SRB assay with IC50 >100 μM. Antiproliferative activity against african green monkey Vero cells assessed by SRB assay with IC50 >100 μM.	42642931

In Vitro

OthersAnti-cancerProtein/Amino Acid Metabolism

Others

S-023-0996 (compound 41a) inhibits EZH2 catalytic activity with an IC₅₀ of 2.41 nM in a cell-free assay and inhibits EGFR WT kinase activity with an IC₅₀ of 42.18 nM; moreover, it shows negligible inhibitory effects on HDAC, HAT, and DNMT in nuclear extracts^[1].
S-023-0996 (10 μM) stabilizes EZH2 and EGFR in CETSA in MDA-MB-468 cells; selectively reduces p-EGFR (Y1068) in EGF-stimulated MDA-MB-231 cells^[1].

Anti-cancer

S-023-0996 exhibits selective antiproliferative activity in HCC1806, MDA-MB-231, MDA-MB-468, and 4T-1 TNBC cells (IC₅₀ 4.25-8.45 μM), while not affecting Vero cells (IC₅₀ >100 μM)^[1].
S-023-0996 (1-2.5 μM; 72 h) maintains dual-target inhibition of EZH2 and EGFR in TNBC cells^[1].
S-023-0996 (1-2.5 μM; 24 h) reduces MDA-MB-231 invasion in the Transwell assay^[1].
S-023-0996 (24 h) most effectively inhibits HCC1806 TNBC cell migration in the wound healing assay^[1].
S-023-0996 (5-10 μM) reduces the viability of TNBC PDO-46 and PDO-47 organoids, with stronger cytotoxicity at 10 μM^[1].

Protein/Amino Acid Metabolism

S-023-0996 induces broader changes in the translational machinery proteome in MDA-MB-231 cells, including 912 uniquely altered proteins and an additional 136 translation-related proteins^[1].
S-023-0996 reduces nascent protein synthesis and decreases puromycin incorporation in MDA-MB-231 cells more effectively than Tazemetostat (HY-13803) + Gefitinib (HY-50895) in the HPG assay^[1].

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

Western Blot Analysis^[1]

Cell Line:

TNBC cells
Concentration:

1 μM; 2.5 μM
Incubation Time:

72 h
Result:

Showed dual-target EZH2 and EGFR inhibition and tumor cell-selective cytotoxic activity.

Cell Invasion Assay^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

1 μM; 2.5 μM
Incubation Time:

24 h
Result:

Resulted in reduced invasion compared with control cells and compared with tazemetostat and gefitinib individually.

Parmacokinetics

Species	Dose	Route	F
Mice^[1]	100 mg/kg	s.c.	19.81 %

In Vivo

Anti-cancer

S-023-0996 (compound 41a) (100 mg/kg; s.c.; every other day; starting day 36 for 24 days) reduces orthotopic MDA-MB-231 TNBC tumor growth and metastatic burden in NSG mice^[1].

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

Animal Model:

NSG (female, 4-6 weeks old, MDA-MB-231 Chili-Luc cells (5 × 10⁶) resuspended in 100 μL PBS mixed with Matrigel in a 1:1 ratio)^[1]
Dosage:

100 mg/kg
Administration:

s.c.; QOD (every other day); starting day 36 for 24 days
Result:

Produced 69% tumor growth inhibition compared with control.
Mean terminal tumor volume was reduced by 268.9 mm3 versus control and by 88.63 mm3 versus the Taz + Gef combination.
Mean terminal tumor weight differed by 0.3062 g versus vehicle.
Reduced metastatic burden compared with the Taz + Gef combination by whole-body bioluminescence imaging in MDA-MB-231 tumor-bearing NSG mice.

Related Protocols :

Chemical Information

Peso molecular 857.05
Fòrmula C₄₉H₆₀N₈O₆
SMILES

O=C1C(CNC(C2=CC(CN3CCN(CCOCCOC4=CC5=C(NC6=CC=CC(C#C)=C6)N=CN=C5C=C4OC)CC3)=CC(N(C7CCOCC7)CC)=C2C)=O)=C(C)C=C(C)N1
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[1]. Satrusal SR, et al. Targeting EZH2 and EGFR therapeutic vulnerabilities of TNBC with a single chemical entity confers preclinical treatment advantage. Molecular therapy : the journal of the American Society of Gene Therapy. 2026 Aug 25.

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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.

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Actividad biológica
- Descripciòn
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureza y Documentación
Referencias

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S-023-0996

Ver todos los productos específicos de isoformas Histone Methyltransferase

Ver todos los productos específicos de isoformas EGFR