Home Cart Sign in  
Chemical Structure| 1951408-58-4 Chemical Structure| 1951408-58-4

Structure of MAK683
CAS No.: 1951408-58-4

Chemical Structure| 1951408-58-4

MAK683

CAS No.: 1951408-58-4

An inhibitor of embryonic ectoderm development protein (EED) and allosteric inhibitor of polycomb repressive complex 2 (PRC2), with potential antineoplastic activity.

Synonyms: EED inhibitor-1

4.5 *For Research Use Only !

Cat. No.: A646657 Purity: 99%

Change View

Size Price

US Stock

Global Stock

In Stock
10mg łďʶÊÊ Inquiry Inquiry
25mg łÇÇî¶ÊÊ Inquiry Inquiry
50mg łËÊǶÊÊ Inquiry Inquiry
100mg ł§Í˶ÊÊ Inquiry Inquiry
250mg łÿóǶÊÊ Inquiry Inquiry
1g łÇÿòď¶ÊÊ Inquiry Inquiry

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 10mg

    łďʶÊÊ

  • 25mg

    łÇÇî¶ÊÊ

  • 50mg

    łËÊǶÊÊ

  • 100mg

    ł§Í˶ÊÊ

  • 250mg

    łÿóǶÊÊ

  • 1g

    łÇÿòď¶ÊÊ

In Stock

- +

US Stock: ship in 0-1 business day
Global Stock: ship in 2 weeks

  • 1-2 Day Shipping
  • High Quality
  • Technical Support
Product Citations

Alternative Products

Product Details of MAK683

CAS No. :1951408-58-4
Formula : C20H17FN6O
M.W : 376.39
SMILES Code : CC1=NC=CC=C1C2=CN=C(NCC3=C4CCOC4=CC=C3F)N5C2=NN=C5
Synonyms :
EED inhibitor-1
MDL No. :MFCD31630846
InChI Key :XLIBABIFOBYHSV-UHFFFAOYSA-N
Pubchem ID :121412508

Safety of MAK683

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of MAK683

epigenetics

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Stromal vascular fraction cells (SVF) 5 μM 5 days Enhanced adipogenic effect PMC11533084
Mesenchymal stem cells C3H10T1/2 5 μM 7 days Promoted lipid accumulation and adipocyte marker expression PMC11533084
Mesenchymal stem cells C3H10T1/2 5 μM 7 days Promoted adipocyte differentiation and increased lipid accumulation PMC11533084
Malignant rhabdoid tumor cells G401 30 nM 7 days Induced adipocyte differentiation and upregulated PPARG and CEBPA expression PMC11533084
Endometrial epithelium cells 0, 20, 40 nM At 40 nM, MAK683 significantly decreased the protein levels of EED, SUZ12 and EZH2, and altered the endometrial receptivity genes (HOXA10, LIF and FOXA2) significantly. Meanwhile, 40 nM MAK683 reduced the H3K27me3 while increasing H3K27ac modification obviously. PMC11814224
Mouse stromal vascular fraction cells 5 μM 5 days Promoted adipocyte differentiation and upregulated adipogenic genes PMC11533084
Malignant rhabdoid tumor cells A204 30 nM 7 days Induced adipocyte differentiation and upregulated adipocyte markers PMC11533084
Malignant rhabdoid tumor cells G401 30 nM 7 days Induced adipocyte differentiation and upregulated PPARG and CEBPA expression PMC11533084

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice TNBC xenograft models Oral 5 μM Twice daily for 28 days To assess the antitumor efficacy of MAK683 in combination with AKT inhibitors in TNBC models, demonstrating that the combination induced significant tumor regression in all models PMC11578877
Mice Pregnant mouse model Uterine horn injection 100 μl (2.7 mg/ml) Single injection, lasting until GD 5.5 MAK683 treatment reduced the thickness of endometrial epithelium, restrained the number of Eed and H3K27me3 positive cells, while decreasing the number of Ck18 positive cells and dramatically increasing the number of Foxa2 and Muc1 positive cells. PMC11814224
Balb/c nude mice G401 xenograft tumors Oral 100 mg/kg Once daily for 21 days Inhibited tumor growth and induced adipocyte differentiation PMC11533084

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02900651 Diffuse Large B-cell Lymphoma Phase 1 Phase 2 Recruiting August 5, 2019 United States, California ... More >> Novartis Investigative Site Recruiting San Francisco, California, United States, 94115 Novartis Investigative Site Recruiting Santa Monica, California, United States, 90404 Contact: Ruth M. Gonzalez       Rngonzalez@mednet.ucla.edu    Principal Investigator: Zev A. Wainberg          United States, Texas Novartis Investigative Site Recruiting Houston, Texas, United States, 77030 Contact: Anna Lui    713-563-4667    alui@mdanderson.org    Principal Investigator: Vivek Subbiah          Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Recruiting Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Recruiting Koeln, Germany, 50937 Hong Kong Novartis Investigative Site Recruiting Hong Kong, Hong Kong Italy Novartis Investigative Site Recruiting Milano, MI, Italy, 20133 Japan Novartis Investigative Site Recruiting Sunto-gun, Shizuoka, Japan, 411-8777 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Spain Novartis Investigative Site Recruiting Madrid, Spain, 28041 Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.28mL

2.66mL

1.33mL

26.57mL

5.31mL

2.66mL

References

 

Historical Records

Categories