A BET bromodomain inhibitor
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Alobresib

Item No. 30726

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-cyclopropyl-5-(3,5-dimethyl-4-isoxazolyl)-α,α-di-2-pyridinyl-1H-benzimidazole-7-methanol
CAS Number
1637771-14-2
Synonyms
  • GS-5829
Molecular Formula
C26H23N5O2
Formula Weight
437.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 10 mM
SMILES
OC(C1=CC=CC=N1)(C2=CC(C3=C(C)ON=C3C)=CC4=C2NC(C5CC5)=N4)C6=CC=CC=N6
InChi Code
InChI=1S/C26H23N5O2/c1-15-23(16(2)33-31-15)18-13-19(24-20(14-18)29-25(30-24)17-9-10-17)26(32,21-7-3-5-11-27-21)22-8-4-6-12-28-22/h3-8,11-14,17,32H,9-10H2,1-2H3,(H,29,30)
InChi Key
CMSUJGUHYXQSOK-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $63

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    5 mg

    $257

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    10 mg

    $481

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    Cayman Chemical
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    Product Description

    Alobresib is an inhibitor of bromodomain and extra-terminal domain (BET) proteins.1,2 It inhibits proliferation of MEC-1 chronic lymphocytic leukemia cells (CLL; IC50 = 46.4 nM).1 Alobresib (400 nM) decreases the levels of Blk and Myc and increases the levels of IκBα in patient-derived CLL cells co-cultured with nurse-like cells (NLC). It inhibits proliferation of USPC-ARK-1 and USPC-ARK-2 uterine serous carcinoma (USC) cells with IC50 values of 31 and 27 nM, respectively.2 Alobresib (10 and 20 mg/kg, p.o.) reduces tumor growth in a USPC-ARK-2 USC mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, E., Hacken, E.T., Sivina, M., et al. The BET inhibitor GS-5829 targets chronic lymphocytic leukemia cells and their supportive microenvironment. Leukemia 34(6), 1588-1598 (2020).

    2. Bonazzoli, E., Predolini, F., Cocco, E., et al. Inhibition of BET bromodomain proteins with GS-5829 and GS-626510 in uterine serous carcinoma, a biologically aggressive variant of endometrial cancer. Clin. Cancer Res. 24(19), 4845-4853 (2018).