For research use only. Not for therapeutic Use.
TP-021 (CAT: I017428) is a potent, orally active B-cell lymphoma 6 (BCL6)-corepressor interaction inhibitor with an IC50 of 0.10 µM in enzyme-linked immunosorbent assay. It demonstrates strong cellular protein–protein interaction inhibition (M2H IC50 = 0.72 µM) without notable cytotoxicity at concentrations up to 30 µM. In a mouse cassette-dosing pharmacokinetic study (0.1 mg/kg iv; 1 mg/kg po), TP-021 displays favorable drug-like properties with oral bioavailability of 79.9%, Cmax of 233 ng/mL, Tmax of 2 h, and MRT of 3.3 h. These attributes make TP-021 a valuable tool compound for studying BCL6-driven oncogenesis and therapeutic targeting.
| CAS Number | 2130878-25-8 |
| Synonyms | 6-[2-chloro-4-nitro-5-(oxan-4-yloxy)anilino]-3,4-dihydro-1H-quinolin-2-one |
| Molecular Formula | C20H20ClN3O5 |
| Purity | ≥95% |
| IUPAC Name | 6-[2-chloro-4-nitro-5-(oxan-4-yloxy)anilino]-3,4-dihydro-1H-quinolin-2-one |
| InChI | InChI=1S/C20H20ClN3O5/c21-15-10-18(24(26)27)19(29-14-5-7-28-8-6-14)11-17(15)22-13-2-3-16-12(9-13)1-4-20(25)23-16/h2-3,9-11,14,22H,1,4-8H2,(H,23,25) |
| InChIKey | RRELDGDKULRRDM-UHFFFAOYSA-N |
| SMILES | C1COCCC1OC2=C(C=C(C(=C2)NC3=CC4=C(C=C3)NC(=O)CC4)Cl)[N+](=O)[O-] |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
