(rac) -Talazoparib
(rac) -Talazoparib ((rac) -BMN-673) (Compound 47) is the orally active inhibitor for PARP1/2 with Ki of 1.2 nM and 0.87 nM. (rac) -Talazoparib inhibits cellular PARylation with an EC50 of 2.51 nM. (rac) -Talazoparib causes the accumulation of DNA damage, inhibits proliferation of BRCA1/2-mutated MX-1 cell and Capan-1 cell with IC50 of 0.3 nM and 5 nM. (rac) -Talazoparib exhibits antitumor efficacy in mouse models[1].
Product Specifications
CAS Number
1207454-56-5
Product Name Alternative
(rac) -BMN-673; (rac) -LT-673
UNSPSC
12352005
Target
PARP
Related Pathways
Cell Cycle/DNA Damage; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Smiles
O=C1NN=C2C(C(NC3=CC(F)=CC1=C32)C4=CC=C(C=C4)F)C5=NC=NN5C
Molecular Formula
C19H14F2N6O
Molecular Weight
380.35
References & Citations
[1]Wang B, et al., Discovery and Characterization of (8S,9R) -5-Fluoro-8- (4-fluorophenyl) -9- (1-methyl-1H-1,2,4-triazol-5-yl) -2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one (BMN 673, Talazoparib), a Novel, Highly Potent, and Orally Efficacious Poly (ADP-ribose) Polymerase-1/2 Inhibitor, as an Anticancer Agent. J Med Chem. 2016 Jan 14;59 (1) :335-57.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PARP1; PARP2
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