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532282 DOT1L Inhibitor, EPZ004777 - CAS 1338466-77-5 - Calbiochem

EPZ004777, DOT1L Inhibitor

DOT1L Inhibitor, EPZ004777 - CAS 1338466-77-5 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: HMTase Inhibitor XVI, EPZ4777, 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)

Primary Target: DOT1L
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      Overview

      Key Spec Table

      CAS #Empirical Formula
      1338466-77-5C₂₈H₄₁N₇O₄
      Description
      Overview

      This product has been discontinued.



      A cell-permeable, non-toxic, a near chemical derivative of S-adenosylmethionine (SAM) that competitively binds to the SAM-binding pocket of DOT1L and inhibits its activity in a reversible manner (IC50 = 400 pM; Ki = 300 pM). Shown to inhibit the methylation of cellular H3K79 in MLL cells and block the expression of leukemogenic genes. Displays excellent selectivity over other histone methyltransferases PRMT5 (IC50 = 521 nM), CARM1, EHMT2, EZH1, EZH2, PRMT1, PRMT8, SETD7 and WHSC1 (IC50 > 50 µM). Inhibits the proliferation of MV4-1, MOLM-13, KOPN-8 cells (IC50 = 170, 720, and 620 nM, respectively) and suppresses the growth of MV4-11 xenografts in nude mice model (50 mg/ml, s.c. minipump infusion). Blocks the cell cycle at G0/G1 phase and induces apoptotic cell death by activating caspase 3/7. Also shown to accelerate reprogramming of somatic cells into induced pluripotent stem cells.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.

      Catalogue Number532282
      Brand Family Calbiochem®
      SynonymsHMTase Inhibitor XVI, EPZ4777, 1-(3-((((2R,3S,4R,5R)-5-(4-Amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl)(isopropyl)amino)propyl)-3-(4-(tert-butyl)phenyl)
      References
      ReferencesDaigle, S.R., et al. 2013. Blood. 122, 1017.
      Yu, W., et al. 2012. Nat. Commun. 3, 1288.
      Daigle, S.R., et al. 2011. Cancer Cell. 20, 53.
      Product Information
      CAS number1338466-77-5
      FormWhite powder
      Hill FormulaC₂₈H₄₁N₇O₄
      Chemical formulaC₂₈H₄₁N₇O₄
      Hygroscopic Hygroscopic
      ReversibleY
      Quality LevelMQ100
      Biological Information
      Primary TargetDOT1L
      Primary Target IC<sub>50</sub>400 pM
      Primary Target K<sub>i</sub>300 pM
      Purity≥97% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage -20°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      532282 0