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    JQ1 Userguide Updated Sept 2011

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    This document provides information about the compound JQ1, including its structural information, storage conditions, in vitro and in vivo study conditions. It details that JQ1 is a bromodomain inhibitor with the chemical name tert-butyl 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepin-6-yl)acetate. It should be stored as a solid at 4°C or below, or as a 10mM DMSO stock at -20°C. For cell

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    JQ1 Userguide Updated Sept 2011

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    This document provides information about the compound JQ1, including its structural information, storage conditions, in vitro and in vivo study conditions. It details that JQ1 is a bromodomain inhibitor with the chemical name tert-butyl 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepin-6-yl)acetate. It should be stored as a solid at 4°C or below, or as a 10mM DMSO stock at -20°C. For cell

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    JQ1 JQ1 Userguide Updated Sept 2011

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    This document provides information about the compound JQ1, including its structural information, storage conditions, in vitro and in vivo study conditions. It details that JQ1 is a bromodomain inhibitor with the chemical name tert-butyl 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepin-6-yl)acetate. It should be stored as a solid at 4°C or below, or as a 10mM DMSO stock at -20°C. For cell

    Copyright:

    Attribution Non-Commercial (BY-NC)
    Download as PDF, TXT or read online from Scribd
    Download as pdf or txt
    10 views2 pages

    JQ1 Userguide Updated Sept 2011

    Uploaded by

    bbddd
    This document provides information about the compound JQ1, including its structural information, storage conditions, in vitro and in vivo study conditions. It details that JQ1 is a bromodomain inhibitor with the chemical name tert-butyl 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepin-6-yl)acetate. It should be stored as a solid at 4°C or below, or as a 10mM DMSO stock at -20°C. For cell

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    James E. Bradner, M.D.

    Division of Hematologic Neoplasia Dana-Farber Cancer Institute Assistant Professor Harvard Medical School 44 Binney Street, Dana 510D Boston, MA 02115 617.632.6629 tel 617.582.7370 fax [email protected] http://bradner.dfci.harvard.edu/

    Compound JQ1 user guide: I. Structural information:

    Compound name: (S)-JQ1, Bromodomain inhibitor (for BRD2, 3, 4, and T)


    Chemical name: tert-butyl 2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3a][1,4]diazepin-6-yl)acetate Chemical Formula: C23HClN4O2S CAS #: 1268524-70-4 Exact Mass: 456.1387 Molecular Weight: 456.9882 SMILES: ClC1=CC=C(C2=N[C@@H](CC(OC(C)(C)C)=O)C3=NN=C(C)N3C4=C2C(C)=C(C)S4)C=C1 Provider: James Bradner Laboratory at Dana-Farber Cancer Institute.

    II. Storage: 1. The compound is more stable for long-term storage as a solid, which should be kept at 4 C minimum although lower temperature storage is highly recommended. 2. The compound can also be converted to 10 mM DMSO stock solution, and kept at -20 C. However, it has been observed that multiple freeze-thaws can cause the decomposition of the compound. III. In vitro study condition: 1. For biological assay: Recommended concentration range from 0.5 nM to 50 M 2. For cell assay: Recommended working concentration with cell assay is 250 nM. IV. In vivo study condition:

    Formulation: 10%HP--CD solution was used as a vehicle which improves the solubility of the compound. The Hydroxypropyl beta cyclodextrin is available at sigma-aldrich (catalog # is C0926-5G at sigmaaldrich.com). The 10% cyclodextrin is prepared in sterile water, which was filtered with 0.22 micron filter. 1. Detailed procedure for dosing the animal: a. We make a concentrated stock of JQ1 in DMSO at a concentration of 50 mg/mL. This is frozen in aliquots sufficient for a single day's dosing (in our case for 20 adult mice). b. Each day, a single vial is thawed at 37 C.

    Teaching Affiliates of Harvard Medical School

    c. 9 parts of 10% cyclodextran is added dropwise while gently vortexing. d. The result is indeed a fine milky solution, but there should not be any visible particles. e. We dose 10 uL/gm of body weight to achieve a final dose of 50 mg/kg. f. We observed that the JQ1 remains active in frozen aliquots. However, repeated cycles of freeze-thaws was not tested and not recommended. g. The animal can also be dosed 100 mg/kg/day or two doses with either 30 or 50 mg/kg. We sincerely hope this information is useful for your study with JQ1. More detailed experimental information can be found in the supporting information of our recent manuscript, (Nature, 2010, 468, 1067-1073). Please feel free to contact us if you have any questions. Sincerely

    James Bradner, M.D.

    Teaching Affiliates of Harvard Medical School

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