A BET bromodomain inhibitor
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BMS 986158

Item No. 27789

Technical Information
Formal Name
3-(1,4-dimethyl-1H-1,2,3-triazol-5-yl)-α,α-dimethyl-5-[(S)-phenyl(tetrahydro-2H-pyran-4-yl)methyl]-5H-pyrido[3,2-b]indole-7-methanol
CAS Number
1800340-40-2
Molecular Formula
C30H33N5O2
Formula Weight
Purity
≥98%
Formulation
A solid
λmax
214, 270, 322 nm
SMILES
CC(O)(C)C(C=C1)=CC2=C1C(N=CC(C3=C(C)N=NN3C)=C4)=C4N2[C@H](C5=CC=CC=C5)C6CCOCC6
InChi Code
InChI=1S/C30H33N5O2/c1-19-28(34(4)33-32-19)22-16-26-27(31-18-22)24-11-10-23(30(2,3)36)17-25(24)35(26)29(20-8-6-5-7-9-20)21-12-14-37-15-13-21/h5-11,16-18,21,29,36H,12-15H2,1-4H3/t29-/m1/s1
InChi Key
KGERZPVQIRYWRK-GDLZYMKVSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BMS 986158 is a BET bromodomain inhibitor with anticancer activity.1 It decreases c-Myc expression and induces cancer cell death in c-Myc-driven cancer cell lines in vitro. BMS 986158 inhibits tumor growth in triple-negative breast, colorectal, and lung cancer patient-derived mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gavai, A.V., Norris, D., Tortolani, D., et alAbstract 5789: Discovery of clinical candidate BMS-986158, an oral BET inhibitor, for the treatment of cancer. Cancer Res. 78(13 Supplement), 5789-5789 (2018).