1373431-65-2
1373431-65-2 structure
- Name: Talazoparib tosylate
- Chemical Name: bmn 673ts
- CAS Number: 1373431-65-2
- Molecular Formula: C26H22F2N6O4S
- Molecular Weight: 552.55200
- Catalog: Signaling Pathways Cell Cycle/DNA Damage PARP
- Create Date: 2016-01-10 18:34:40
- Modify Date: 2025-09-10 10:32:47
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Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1.
| Name | bmn 673ts |
|---|---|
| Synonyms |
Talazoparib tosylate
UNII-02WK9U5NZC (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-2,7,8,9-tetrahydro-3H-pyrido(4,3,2-de)phthalazin-3-one MONO(4-methylbenzenesulfonate) Talazoparib tosylate [USAN] 3H-Pyrido(4,3,2-de)phthalazin-3-one,5-fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-,(8S,9R)-,4-methylbenzenesulfonate (1:1) |
| Description | Talazoparib tosylate (BMN 673ts) is a novel, potent and orally available PARP1/2 inhibitor with an IC50 of 0.57 nM for PARP1. |
|---|---|
| Related Catalog | |
| Target |
IC50: 0.57 nM (PARP1)[1] |
| 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[1]. |
| 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[1]. |
| Cell Assay | LoVo cells are treated with Talazoparib (10, 40 nM) and temozolomide (TMZ) either alone or in combination for 5 days. Surviving fraction is determined using CellTiter-Glo assay.[1] |
| Animal Admin | Mice[1] In single-agent studies, olaparib (100 mg/kg), Talazoparib (0.33 or 0.1 mg/kg/d), or vehicle (10% DMAc, 6% Solutol, and 84% PBS) is administered by oral gavage (per os), once daily or Talazoparib (0.165 mg/kg) twice daily for 28 consecutive days. Mice are continuously monitored for 10 more days after last day of dosing[1]. |
| References |
| Molecular Formula | C26H22F2N6O4S |
|---|---|
| Molecular Weight | 552.55200 |
| Exact Mass | 552.13900 |
| PSA | 154.73000 |
| LogP | 4.22080 |
| Storage condition | 2-8℃ |
| Precursor 0 | |
|---|---|
| DownStream 1 | |
