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Talazoparib

Chemical Structure : Talazoparib

CAS No.: 1207456-01-6

Talazoparib (BMN-673, LT-673)

Catalog No.: PC-23876Not For Human Use, Lab Use Only.

Talazoparib (MN 673) is a highly potent, selective PARP1/2 inhibitor (PARP1, IC50=0.57 nM), inhibits PARP1 and PARP2 to a similar extent with Ki of 1.20 and 0.85 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Talazoparib (MN 673) is a highly potent, selective PARP1/2 inhibitor (PARP1, IC50=0.57 nM), inhibits PARP1 and PARP2 to a similar extent with Ki of 1.20 and 0.85 nM, respectively.
Talazoparib (MN 673) inhibits intracellular poly (ADP-ribose) (PAR) formation with an IC50 of 2.5 nM in LoVo cells to hydrogen peroxide (H2O2) to induce PAR synthesis.
Talazoparib (MN 673) shows no effect on PARG activity as well as a protein panel.
Talazoparib (MN 673) selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects。
Talazoparib (MN 673) elicited remarkable antitumor activity in vivo xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency。

Physicochemical Properties

M.Wt 380.36
Formula C19H14F2N6O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one

References

1. Smith MA, et al. Clin Cancer Res. 2015 Feb 15;21(4):819-32.

2. Shen Y, et al. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.

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