Veliparib (ABT-888)

ArtNr	S1004-5000
Hersteller	Selleckchem
CAS-Nr.	912444-00-9
Menge	5 g
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 50 mg 5 g
Kategorie	Oncology Inhibitors & Compound Libraries Small Molecules By Organ Lung Cancer Bladder Cancer Colorectal Cancer Breast Cancer Testicular & Prostate Cancer
Typ	Inhibitors
Specific against	other
Smiles	CC1(CCCN1)C2=NC3=C(C=CC=C3N2)C(=O)N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	NSC 737664
Similar products	ABT-888
Lieferbar
Manufacturer - Targets	PARP2, PARP1
Storage Conditions	2 years -80 in solvent
Molecular Weight	244, 29
Administration	Orally administered
Animal Models	NCI-H460, H460, B16F10 and 9L xenografts in C57BL/6 mice
Clinical Trials	A Phase I study of evaluating the bioavailability and food effect of three formulations of ABT-888 on pharmacokinetics in subjects with solid tumors has been completed.
Dosages	ca.25 mg/kg
Formulation	Formulated in solution containing 0.9% NaCl adjusted to pH 4.0
IC50	5.2 nM (Ki), 5.2 nM (Ki), 5.2 nM (Ki), 5.2 nM (Ki), 5.2 nM (Ki), 5.2 nM (Ki)
In vitro	ABT-888 is inactive to SIRT2 (>5 uM). [1] ABT-888 inhibits the PARP activity with EC50 of 2 nM in C41 cells. [2] 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. [3] ABT-888 also inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. ABT-888 (10 uM) 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. [4]
In vivo	The oral bioavailability of ABT-888 is 56%-92% in mice, Sprague-Dawley rats, beagle dogs, and cynomolgus monkeys after oral administration. [1] 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. [3] 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. [4]
Kinase Assay	In vitro PARP assays, PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 uM [3H]NAD+ (1.6 uCi/mmol), 200 nM biotinylated histone H1, 200 nM slDNA, and 1 nM PARP-1 or 4 nM PARP-2 enzyme. Reactions are terminated with 1.5 mM benzamide, transferred to streptavidin Flash plates, and counted using a TopCount microplate scintillation counter.
Solubility (25C)	DMSO 17 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	Veliparib (ABT-888, NSC 737664) is a potent inhibitor of PARP1 and PARP2 with Ki 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.
Chemical Name	(R)-2-(2-methylpyrrolidin-2-yl)-1H-benzo[d]imidazole-4-carboxamide
Features	ABT-888 is developed to increase the effectiveness of common cancer therapies such as radiation and alkylating agents.

Hinweis: Die dargestellten Informationen und Dokumente (Bedienungsanleitung, Produktdatenblatt, Sicherheitsdatenblatt und Analysezertifikat) entsprechen unserem letzten Update und sollten lediglich der Orientierung dienen. Wir übernehmen keine Garantie für die Aktualität. Für spezifische Anforderungen bitten wir Sie, uns eine Anfrage zu stellen.

Alle Produkte sind nur für Forschungszwecke bestimmt. Nicht für den menschlichen, tierärztlichen oder therapeutischen Gebrauch.

Arbeitsanleitung (Data Sheet) anfordern

S1004-5000-datasheet.pdf

S1004-5000-safety-datasheet.pdf