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EPZ-5676

A potent DOT1L inhibitor
Catalog #: 2382
SKU-Size Size Price Qty
2382-1 1 mg
$125.00
2382-5 5 mg
$495.00
More Sizes Get Quote

Product Details

Alternate Name (2R,3R,4S,5R)-2-(6-amino-9H-purin-9-yl)-5-((((1r,3S)-3-(2-(5-(tert-butyl)-1H-benzo[d]imidazol-2-yl)ethyl)cyclobutyl)(isopropyl)amino)methyl)tetrahydrofuran-3,4-diol
Appearance Crystalline solid
CAS # 1380288-87-8
Molecular Formula C₃₀H₄₂N₈O₃
Molecular Weight 562.71
Purity ≥98% by HPLC
Solubility DMSO (~ 25 mg/ml)
SMILES CC(C)(C)C1=CC2=C(NC(CC[[email protected]]3C[[email protected]@H](N(C[[email protected]@H]4[[email protected]@H](O)[[email protected]@H](O)[[email protected]](N5C(N=CN=C6C6N)=C6N=C5)O4)C(C)C)C3)=N2)C=C1
InChi InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17-,19+,22-,25-,26-,29-/m1/s1
InChi Key LXFOLMYKSYSZQS-LURJZOHASA-N
Handling Protect from light and air
Storage Conditions -20 ̊C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

A potent and selective inhibitor of DOT1L methyltransferase (Ki = 80 pM). EPZ-5676 displays 37,000-fold selectivity over all other tested methyltransferases. It inhibits H3K79 methylation and MLL-fusion target gene expression and displays potent cell killing selective for acute leukemia lines bearing MLL translocations.


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