Veliparib (ABT-888) - Moligand™, 10mM in DMSO , PARP 1, 2 and 3 inhibitor, CAS No.912444-00-9, PARP 1, 2 and 3 inhibitor

CAS: 912444-00-9 Cat. No.: V408786 Peso molecular: 244.3 Número EC: 681-636-1 PubChem CID: 11960529

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NSC 737664 | (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Veliparib (ABT-888, NSC 737664) is a potent inhibitor ofPARP1andPARP2withKiof 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increasesautophagyandapoptosis. Phase 3.
In vitro

ABT-888 is inactive to SIRT2 (>5 μM). ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. ABT-888 could decrease the PAR levels in both irradiated and nonirradiated H460 cells. ABT-888 also reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. ABT-888 increases apoptosis and autophagy in H460 cells when combination with radiation. ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. ABT-888 shows effective radiosensitivity in oxic H1299 cells. Furthermore, ABT-888 could attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1.

In vivo

The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. ABT-888 (25 mg/kg i.p.) could improve tumor growth delay in a NCI-H460 xenograft model with well tolerated. Combination with radiation, ABT-888 decreases the tumor vessel formation. ABT-888 reduces intratumor PAR levels by more than 95% at a dose of 3 and 12.5 mg/kg in A375 and Colo829 xenograft models and the suppression could be maintained over time.
Cell Data

cell lines：ConA-stimulated T cells and LPS-stimulated B cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

NSC 737664 | (R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with K_i of 5.2 nM and 2.9 nM in cell-free assays, respectively. It is inactive to SIRT2. Veliparib increases autophagy and apoptosis. 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

PARP 1, 2 and 3 inhibitor

Propiedades del producto

• ALogP: 0.5

Nombres e identificadores

• Isómeros SMILES: C[C@@]1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
• PubChem CID: 11960529
• Peso molecular: 244.3

Objetivos asociados (humanos)

PARP1 Tclin Poly [ADP-ribose] polymerase 1 (27 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 (9 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: 81 mg/mL (198.83 mM); Ethanol: 4 mg/mL (9.81 mM); Water: Insoluble