(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one
CAS: 1207456-01-6
Molecular Formula: C19H14F2N6O
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673 - Names and Identifiers
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673 - Physico-chemical Properties
| Molecular Formula | C19H14F2N6O |
| Molar Mass | 380.35 |
| Density | 1.63 |
| Melting Point | 247 - 249°C |
| Solubility | DMSO (Slightly), Methanol (Slightly) |
| Appearance | Solid |
| Color | White to Off-White |
| pKa | 10.14±0.60(Predicted) |
| Storage Condition | Hygroscopic, -20°C Freezer, Under inert atmosphere |
| In vitro study | BMN-673 selectively binds to PARP and inhibits PARP-mediated repair of single-stranded DNA breaks through the base excision repair pathway. It enhances the accumulation of DNA strand breaks, promotes genomic instability, and ultimately leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 acts on cells with BRCA-1 mutation (MX-1,IC50=0.3 nM) and BRCA-2 mutation (Capan-1,IC50=5 nM), and has single-agent cytotoxicity. In contrast, BMN-673 acted on MRC-5 normal human fibroblasts and other tumor cell lines containing wild-type BRCA-1 and BRCA-2 genes, with an IC50 of 90 nM to 1.9 μm. BMN 673 also significantly enhanced the cytotoxic effects of Temozolomide and SN-38 on cultured human cancer cells. |
| In vivo study | In pharmacokinetic studies in rats, BMN673 was dosed alone daily with> 50% oral bioavailability and pharmacokinetic properties. In a MX-1 xenograft tumor model study, daily oral administration of BMN 673 significantly enhanced the antitumor effect of cytotoxic therapy in a dose-dependent manner. |
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673 - Introduction
BMN 673 is a new type of PARP inhibitor. IC50 is 0.58 nM. It also effectively inhibits PARP-2, but does not inhibit PARG. It is highly sensitive to PTEN mutation.
Last Update：2022-10-16 17:12:43
(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673 - Reference Information
| biological activity | Talazoparib (BMN 673) is a new type of PARP inhibitor with IC50 of 0.58 nM, which also effectively inhibits PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3. Talazoparib (BMN 673, LT-673) is a new type of PARP inhibitor. the IC50 of PARP1 in cell-free test is 0.57 nM. It is also a potent PARP-2 inhibitor but does not inhibit PARG and is highly sensitive to PTEN mutants. Phase 3. |
| features | the most effective selective PARP inhibitor reported so far. |
| Target | Value |
| PARP1 (Cell-free assay) | 0.57 nM |
Last Update：2024-04-09 20:49:11
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Spot supply
Product Name: Talazoparib (BMN 673) Visit Supplier Webpage Request for quotationCAS: 1207456-01-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Spot supply
Product Name: (8S,9R)-BMN 673 Visit Supplier Webpage Request for quotationCAS: 1207456-01-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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