A Bcl-6 degrader
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BI-3802

Item No. 41731

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
rel-2-[[6-[[5-chloro-2-[(3R,5S)-3,5-dimethyl-1-piperidinyl]-4-pyrimidinyl]amino]-1,2-dihydro-1-methyl-2-oxo-3-quinolinyl]oxy]-N-methyl-acetamide
CAS Number
2166387-65-9
Molecular Formula
C24H29ClN6O3
Formula Weight
485.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CN1C2=CC=C(NC3=NC(N4C[C@H](C[C@H](C4)C)C)=NC=C3Cl)C=C2C=C(C1=O)OCC(NC)=O
InChi Code
InChI=1S/C24H29ClN6O3/c1-14-7-15(2)12-31(11-14)24-27-10-18(25)22(29-24)28-17-5-6-19-16(8-17)9-20(23(33)30(19)4)34-13-21(32)26-3/h5-6,8-10,14-15H,7,11-13H2,1-4H3,(H,26,32)(H,27,28,29)/t14-,15+
InChi Key
GXTJETQFYHZHNB-GASCZTMLSA-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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    Cayman Chemical
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    Product Description

    BI-3802 is a degrader of Bcl-6 with a half-maximal degradation concentration (DC50) value of 20 nM in SU-DHL-4 B cell lymphoma cells.1 It binds to Bcl-6 in a cell-free assay and inhibits the interaction of Bcl-6 with nuclear receptor co-repressor 1 (NCOR1) in a reporter assay (IC50s = ≤3 and 43 nM, respectively). BI-3802 induces Bcl-6 polymerization, as well as SIAH1-dependent ubiquitination of Bcl-6, in cell-free assays.2 It induces expression of the Bcl-6 target genes PTPN6 and RAPGEF1 in SU-DHL-4 cells in a concentration- and time-dependent manner.1 BI-3802 enhances decreases in tumor volume and weight induced by the c-Abl, Bcr-Abl, PDGFR, and c-Kit inhibitor imatinib (Item No. 13139) in a GIST-T1 gastrointestinal stromal tumor mouse xenograft model.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kerres, N., Steurer, S., Schlager, S., et al. Chemically induced degradation of the oncogenic transcription factor BCL6. Cell. Rep. 20(12), 2860-2875 (2017).

    2. Słabicki, M., Yoon, H., Koeppel, J., et al. Small-molecule-induced polymerization triggers degradation of BCL6. Nature 588(7836), 164-168 (2020).

    3. Zeng, X., Zhao, F., Jia, J., et al. Targeting BCL6 in gastrointestinal stromal tumor promotes p53-mediated apoptosis to enhance the antitumor activity of imatinib. Cancer Res. 83(21), 3624-3635 (2023).