A degrader of Bcl-6
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Product Type

Biochemicals

Research Area

Cancer

CCT369260

Item No. 41314

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
rel-5-[[5-chloro-2-[(3R,5S)-4,4-difluoro-3,5-dimethyl-1-piperidinyl]-4-pyrimidinyl]amino]-1,3-dihydro-3-(3-hydroxy-3-methylbutyl)-1-methyl-2H-benzimidazol-2-one
CAS Number
2253878-44-1
Molecular Formula
C24H31ClF2N6O2
Formula Weight
509.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/ml
SMILES
C[C@@H]1CN(C(N=C2NC(C=C3N4CCC(C)(C)O)=CC=C3N(C)C4=O)=NC=C2Cl)C[C@H](C)C1(F)F
InChi Code
InChI=1S/C24H31ClF2N6O2/c1-14-12-32(13-15(2)24(14,26)27)21-28-11-17(25)20(30-21)29-16-6-7-18-19(10-16)33(22(34)31(18)5)9-8-23(3,4)35/h6-7,10-11,14-15,35H,8-9,12-13H2,1-5H3,(H,28,29,30)/t14-,15+
InChi Key
VFNPUAOAEFMXQI-GASCZTMLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $215

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    10 mg

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    25 mg

    $644

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    50 mg

    $1,073

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    Cayman Chemical
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    Product Description

    CCT369260 is a degrader of Bcl-6.1 It induces degradation of Bcl-6 in SU-DHL-4, OCI-LY1, and Karpas-422 cells with half-maximal degradation concentration (DC50) values of 0.09, 0.049, and 0.062 µM, respectively. CCT369260 inhibits the growth of SU-DHL-4, OCI-LY1, and OCI-Ly3 cancer cells (GI50s = 0.092, 0.035, and 1.6 µM, respectively). It reduces intratumoral Bcl-6 levels in an OCI-LY1 lymphoma mouse xenograft model for up to ten hours after administration of a 15 mg/kg dose.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bellenie, B.R., Cheung, K.-M.J., Varela, A., et al. Achieving in vivo target depletion through the discovery and optimization of benzimidazolone BCL6 degraders. J. Med. Chem. 63(8), 4047-4068 (2020).