Talazoparib (BMN 673) - Moligand™, 10mM in DMSO , Inhibitor of poly(ADP-ribose) polymerase 1;Inhibitor of poly(ADP-ribose) polymerase 2, CAS No.1207456-01-6, Inhibitor of poly(ADP-ribose) polymerase 1;Inhibitor of poly(ADP-ribose) polymerase 2

CAS: 1207456-01-6 Cat. No.: T408458 Peso molecular: 380.35 Número EC: 815-271-8

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

LT-673 | 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)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Talazoparib (BMN 673, LT-673) is a novelPARPinhibitor withIC50of 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.
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. 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.

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.
Cell Data

cell lines：MCF-7 breast cancer cells

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

LT-673 | 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)-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

Inhibitor of poly(ADP-ribose) polymerase 1;Inhibitor of poly(ADP-ribose) polymerase 2

Propiedades del producto

• ALogP: 2.3

Nombres e identificadores

• Isómeros SMILES: CN1C(=NC=N1)[C@@H]2[C@H](NC3=CC(=CC4=C3C2=NNC4=O)F)C5=CC=C(C=C5)F
• CAS alternativo: 1207456-01-6,1373431-65-2
• Términos de entrada MeSH: BMN 673;BMN-673;BMN673;talazoparib;Talzenna
• Peso molecular: 380.35
• Reaxy-Rn: 19918515
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=19918515&ln=

Objetivos asociados (humanos)

PARP1 Tclin Poly [ADP-ribose] polymerase 1 (9 Activities)

Discover Target: PARP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PARP2 Tclin Poly [ADP-ribose] polymerase 2 (3 Activities)

Discover Target: PARP2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Propiedades químicas y físicas

• Solubilidad: Solubility (25°C) In vitro DMSO: Insoluble; Water: Insoluble; Ethanol: Insoluble