Talazoparib tosylate

CAS No. 1373431-65-2

Talazoparib tosylate( —— )

Catalog No. M33505 CAS No. 1373431-65-2

Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Talazoparib tosylate
  • Note
    Research use only, not for human use.
  • Brief Description
    Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1).
  • Description
    Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
  • In Vitro
    Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC50=0.57 nM), it has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant (KD) of 0.29 nM. Talazoparib inhibits PARP1 and -2 to a similar extent, with Kis of 1.20 and 0.85 nM, respectively. Talazoparib selectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-fold greater potency than existing PARP1/2 inhibitors. Talazoparib targets tumor cells with homologous recombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM.
  • In Vivo
    Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity; xenografted tumors that carry defects in DNA repair due to BRCA mutations or PTEN deficiency are profoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additive antitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs.
  • Synonyms
    ——
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    PARP
  • Recptor
    PARP
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1373431-65-2
  • Formula Weight
    552.55
  • Molecular Formula
    C26H22F2N6O4S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : ≥ 108 mg/mL (195.46 mM) H2O : < 0.1 mg/mL (insoluble)
  • SMILES
    Cc1ccc(cc1)S(O)(=O)=O.Cn1ncnc1[C@@H]1[C@H](Nc2cc(F)cc3c2c1n[nH]c3=O)c1ccc(F)cc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Shen Y, et al. BMN 673, a novel and highly potent PARP1/2 inhibitor for the treatment of human cancers with DNA repair deficiency. Clin Cancer Res. 2013 Sep 15;19(18):5003-15.?
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