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CCT373566

Chemical Structure : CCT373566

CAS No.: 2378853-66-6

CCT373566

Catalog No.: PC-38807Not For Human Use, Lab Use Only.

CCT373566 is a highly potent, in vivo active BCL6 degarder with IC50 of 2.2 nM and DC50 of 0.7 nM in TR-FRET and cellular BCL6 degradation assays, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CCT373566 is a highly potent, in vivo active BCL6 degarder with IC50 of 2.2 nM and DC50 of 0.7 nM in TR-FRET and cellular BCL6 degradation assays, respectively.
CCT373566 exhibits potent growth inhibition in 14-day proliferative assays of BCL6 dependent DLBCL cell lines, HT, Karpas 422, SU-DHL-4 (GI50 values, 1.4-12.5 nM), but not in the BCL6 low-expressing cell line OCI-Ly3.
CCT373566 is a useful probe suitable for sustained depletion of BCL6 in vivo.
CCT373566 (50 mg/kg, BID) showed modest in vivo efficacy in a lymphoma xenograft mouse model following oral dosing

Physicochemical Properties

M.Wt 547.004
Formula C26H29ClF2N6O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-10-((5-Chloro-2-((3R,5S)-3-hydroxy-5-methylpiperidin-1-yl)pyrimidin-4-yl)amino)-2-cyclopropyl-3,3-difluoro-7-methyl-1,2,3,4-tetrahydro-[1,4]oxazepino[2,3-c]quinolin-6(7H)-one

References

1. Rosemary Huckvale, et al. J Med Chem. 2022 Jun 2. doi: 10.1021/acs.jmedchem.1c02175.

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