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Home > Products >  Talazoparib (BMN 673)

Talazoparib (BMN 673) CAS NO.1207456-01-6

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Keywords

  • Talazoparib (BMN 673)
  • LT-673
  • 1207456-01-6

Quick Details

  • ProName: Talazoparib (BMN 673)
  • CasNo: 1207456-01-6
  • Molecular Formula: C19H14F2N6O
  • ProductionCapacity: Metric Ton/Day
  • Purity: >97%
  • LimitNum: 0 Metric Ton

Superiority

Biological Activity

Description Talazoparib (BMN 673, LT-673) is a novel PARP inhibitor with IC50 of 0.57 nM for PARP1 in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Features Most potent and selective PARPi reported thus far.
Targets
PARP1 [1]
(Cell-free assay)
0.57 nM
In vitro

BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM. [1] In cultured human cancer cells, BMN 673 also significantly enhances the cytotoxic efficacy of both Temozolomide and SN-38. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors. [2]

Cell Data
 
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BR5FVB1-Akt Growth Inhibition Assay 0.1-100 nM 24/48/72 h   inhibits cell proliferation dose dependently 26047697
BR5FVB1-Akt Apoptosis Assay 0.1-100 nM 72 h   induces apoptosis 26047697
Capan-1 Growth Inhibition Assay       IC50=16.0 ± 5.4 µM  25864590

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot       29158830 28947502 28167507 30472087
Growth inhibition assay 29158830
Immunofluorescence   28958991 30621214
In vivo In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner. [2]

 

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