talazoparib tosylate
Talazoparib is an inhibitor of poly (ADP-ribose) polymerase (PARP) enzymes, including PARP1 and PARP2, which play a role in DNA repair. In vitro studies with cancer cell lines that harbored defects in DNA repair genes, including BRCA 1 and 2, have shown that talazoparib-induced cytotoxicity may involve inhibition of PARP enzymatic activity and increased formation of PARP-DNA complexes resulting in DNA damage, decreased cell proliferation, and apoptosis. Talazoparib anti-tumor activity was observed in human patient-derived xenograft breast cancer tumor models that expressed mutated or wild-type BRCA 1 and 2.
Ligand Summary
UNII: 9QHX048FRV
PubChem: 135565082
ChEMBL: CHEMBL3137320
DrugCentral: 5300
LyCHI: FRY8HJ82KBTN
Target Activities
PARP1
Poly [ADP-ribose] polymerase 1
8 Activities
Items per page:
1 – 8 of 8
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 9.24 | J. Med. Chem., (2016) 59:1:335 | ||||
IC50 | 9.24 | Bioorg Med Chem Lett, (2016) 26:16:4127 | ||||
IC50 | 9.24 | Eur J Med Chem, (2019) 165:None:198 | ||||
IC50 | 9.22 | J. Med. Chem., (2015) 58:8:3302 | ||||
Ki | 8.92 | J. Med. Chem., (2016) 59:1:335 | ||||
Ki | 8.92 | Eur J Med Chem, (2019) 165:None:198 | ||||
IC50 | 8.14 | Eur J Med Chem, (2017) 138:None:514 | ||||
Ki | 8.92 | INHIBITOR | ||||
PARP2
Poly [ADP-ribose] polymerase 2
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.07 | J. Med. Chem., (2016) 59:1:335 | ||||
Ki | 9.05 | Eur J Med Chem, (2019) 165:None:198 | ||||
Ki | 9.06 | INHIBITOR | ||||