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Chemical Structure| 1338466-77-5 Chemical Structure| 1338466-77-5

Structure of EPZ004777
CAS No.: 1338466-77-5

Chemical Structure| 1338466-77-5

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EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates > 1,200-fold selectivity for DOT1L over all other tested PMTs.

Synonyms: EPZ004777

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Product Details of EPZ004777

CAS No. :1338466-77-5
Formula : C28H41N7O4
M.W : 539.67
SMILES Code : O=C(NC1=CC=C(C(C)(C)C)C=C1)NCCCN(C[C@H]2O[C@@H](N3C=CC4=C(N)N=CN=C43)[C@H](O)[C@@H]2O)C(C)C
Synonyms :
EPZ004777
MDL No. :MFCD25563264
InChI Key :WXRGFPHDRFQODR-ICLZECGLSA-N
Pubchem ID :56962336

Safety of EPZ004777

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

Related Pathways of EPZ004777

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

    DOT1L, IC50:0.4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MLL-AF10 and CALM-AF10 transformed LSK cells 10 µM 2 weeks To test the effect of EPZ004777 on the colony forming ability, results showed significantly fewer compact colonies were formed. PMC3932800

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MLL-AF10 and CALM-AF10 transformed cells Injection 10 µM 2 weeks To assess the spleen-colony forming ability post-treatment, results showed that treated cells failed to form any large spleen colonies. PMC3932800

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.85mL

0.37mL

0.19mL

9.26mL

1.85mL

0.93mL

18.53mL

3.71mL

1.85mL

References

 

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