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Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $44 | 7-10 days |
Description | Talazoparib tosylate is a novel and potent PARP1/2 (n IC50: 0.57 nM for PARP1). |
In vitro | Talazoparib inhibits PARP1 and -2 to a similar extent (Kis: 1.20 and 0.85 nM, respectively). Talazoparib induces nuclear γ-H2AX foci at concentrations as low as 100 pM. Talazoparib has no effect on PARG activity at concentrations up to 1 μM. Talazoparib binds to PARP1 with a dissociation constant of 0.29 nM. 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 or BRCA2-deficient are profoundly sensitive to Talazoparib. [1]. |
In vivo | Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosed in carboxymethyl cellulose. Talazoparib (p.o.) 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 [1]. |
Alias | BMN 673ts |
Molecular Weight | 552.55 |
Formula | C26H22F2N6O4S |
Cas No. | 1373431-65-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 108 mg/mL (195.46 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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