Talazoparib | PARP inhibitor

CAS:
 1207456-01-6
Catalog Number:
 10-5461
Talazoparib chemical structure

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Talazoparib (1207456-01-6) is a PARP1/2 (poly ADP ribose polymerase) inhibitor with higher potency than olaparib (IC50 = 0.6 and 1-5 nM, respectively).1,2 Because PARP is essential for single-stranded DNA repair (which is used more frequently by tumor cells than normal cells), talazoparib interferes with tumor cell function and division, causing cytotoxic death.1 Traps PARP where it is bound on DNA, further interfering with cellular replication.3 However, PARP trapping might also lead to death of normal cells3, possibly through induction of DNA damage.4 Clinically useful for mutant BRCA1/2, HER2-negative breast cancer.5

References/Citations:

  1. Shen et al. (2013) BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency; Clin. Cancer Res. 19 5003
  2. Menear et al. (2008) 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1; J. Med. Chem. 51 6581
  3. Hopkins et al. (2019) PARP1 Trapping by PARP Inhibitors Drives Cytotoxicity in Both Cancer Cells and Healthy Bone Marrow; Mol. Cancer Res. 17 409
  4. Sinha et al. (2021) PARP-DNA trapping ability of PARP inhibitors jeopardizes astrocyte viability: Implications for CNS disease therapeutics; Neuropharmacology 187 108502
  5. Eskiler et al. (2019) Talazoparib to treat BRCA-positive breast cancer; Drugs Today (Barc.) 55 459
1207456-01-6, BMN673, BMN673 supplier, PARP inhibitor, PARP1/2 inhibitor, talazoparib, Talazoparib supplier
CAS:
1207456-01-6
Catalog Number:
10-5461
Activity:
PARP inhibitor
Chemical Names:
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazin-3-one
Alternate Name:
BMN673
Molecular Weight:
380.36
Molecular Formula:

C19H14F2N6O

Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
White solid
Purity:

>97% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Download Product Data Sheet

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Talazoparib (1207456-01-6) is a PARP1/2 (poly ADP ribose polymerase) inhibitor with higher potency than olaparib (IC50 = 0.6 and 1-5 nM, respectively).1,2 Because PARP is essential for single-stranded DNA repair (which is used more frequently by tumor cells than normal cells), talazoparib interferes with tumor cell function and division, causing cytotoxic death.1 Traps PARP where it is bound on DNA, further interfering with cellular replication.3 However, PARP trapping might also lead to death of normal cells3, possibly through induction of DNA damage.4 Clinically useful for mutant BRCA1/2, HER2-negative breast cancer.5

References/Citations:

  1. Shen et al. (2013) BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency; Clin. Cancer Res. 19 5003
  2. Menear et al. (2008) 4-[3-(4-Cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: A Novel Bioavailable Inhibitor of Poly(ADP-ribose) Polymerase-1; J. Med. Chem. 51 6581
  3. Hopkins et al. (2019) PARP1 Trapping by PARP Inhibitors Drives Cytotoxicity in Both Cancer Cells and Healthy Bone Marrow; Mol. Cancer Res. 17 409
  4. Sinha et al. (2021) PARP-DNA trapping ability of PARP inhibitors jeopardizes astrocyte viability: Implications for CNS disease therapeutics; Neuropharmacology 187 108502
  5. Eskiler et al. (2019) Talazoparib to treat BRCA-positive breast cancer; Drugs Today (Barc.) 55 459