CCT369260 (compound 1) is an orally avtive B-cell lymphoma 6 (BCL6) inhibitor with anti-tumor activity. CCT369260 (compound 1) exhibits an IC 50 of 520 nM
In Vivo
CCT369260 (compound 1, 15 mg/kg, po, single dose) significantly inhibits BCL6 in OCI-Ly1 DLBCL xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: OCI-Ly1 DLBCL xenograft model (female SCID mice) . Dosage: 15 mg/kg. Administration: PO, single dose. Result: Decreased the levels of BCL6 in the tumor observed up to 10 h after administration. Animal Model: Female Balb/C mice . Dosage: 1 mg/kg iv and 5 mg/kg po (Pharmacokinetic Analysis). Administration: IV and PO Result: Demonstrated moderate clearance (CL 20 mL min −1 kg −1 ) with mean oral bioavailability of 54%.