A BET family protein inhibitor
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INCB 057643

Item No. 31456

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
8-(6,7-dihydro-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-2,2,4-trimethyl-6-(methylsulfonyl)-2H-1,4-benzoxazin-3(4H)-one
CAS Number
1820889-23-3
Molecular Formula
C20H21N3O5S
Formula Weight
415.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
λmax
226, 257 nm
SMILES
O=C1C2=C(C(C3=C(OC(C)(C)C(N4C)=O)C4=CC(S(C)(=O)=O)=C3)=CN1C)C=CN2
InChi Code
InChI=1S/C20H21N3O5S/c1-20(2)19(25)23(4)15-9-11(29(5,26)27)8-13(17(15)28-20)14-10-22(3)18(24)16-12(14)6-7-21-16/h6-10,21H,1-5H3
InChi Key
VZSAMEOETVNDQH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    25 mg

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    Product Description

    INCB 057643 is a bromodomain and extra terminal domain (BET) family protein inhibitor.1 It inhibits binding of bromodomain-containing protein 2 (BRD2), BRD3, and BRD4 to an acetylated histone H4 peptide in vitro. INCB 057643 decreases Myc levels in, and inhibits proliferation of, acute myeloid leukemia (AML), diffuse large B cell lymphoma (DLBCL), and multiple myeloma (MM) cells. In vivo, INCB 057643 reduces tumor growth in AML, DLBCL, and MM mouse xenograft models. It also reduces tumor growth when administered alone or in combination with docetaxel (Item No. 11637) or enzalutamide (Item No. 11596) in a 22Rv1 castration-resistant prostate cancer (CRPC) mouse xenograft model.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stubbs, M.C., Maduskuie, T., Burn, T., et al. Abstract 5071: Preclinical characterization of the potent and selective BET inhibitor INCB057643 in models of hematologic malignancies. AACR Cancer Res. 77(13), 5071 (2017).

    2. Vázquez, R., Civenni, G., Zoppi, G., et al. Abstract 5793: Anti-tumor efficacy of INCB057643, a novel BET bromodomain inhibitor, in castration-resistant prostate cancer as single agent and in combination therapy. AACR Cancer Res. 78(13Supp), 5793-5793 (2018).