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Talazoparib

CAT: 0013-GTR19164305-01Size: 500 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19164305-01Size:500 mg
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Description
Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. (In Vitro) :Talazoparib shows an EC50 of 2.51 nM in cellular PARylation assay.Talazoparib shows EC50s of 0.3 nM, 5 nM and 0.31 for MX-1 cells (BRCA1 mutant), Capan-1 cells (BRCA2 mutant) and MRC-5 cells (normal) . (In Vivo) :Talazoparib (0.33 mg/kg; i.g.; once daily; for 28 days) exhibits antitumor activity against BRCA1 mutant breast cancer model in mice.Talazoparib exhibits moderate oral bioavailability (rat 56%) and Cmax (rat 7948 ng/mL) following oral administration (rat 10 mg/kg) . Talazoparib exhibits the terminal elimination half-life (rat 2.25 h) due to plasma clearance (2 mL/min/kg) following intravenous administration (rat 5 mg/kg) .
CAS Number
1207456-01-6
Product Name Alternative
BMN 673
Purity
>98% (HPLC)
Solubility
DMSO:38 mg/mL warmed (99.9 mM) ; Ethanol:<1 mg/mL (<1 mM) ; Water:<1 mg/mL (<1 mM)
Smiles
CN1C (=NC=N1) [C@@H]2[C@H] (N=C3C=C (C=C4C3=C2NNC4=O) F) C5=CC=C (C=C5) F
Molecular Formula
C19H14F2N6O
Molecular Weight
380.35
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.

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