Product Introduction
Bioactivity


英文名: Veliparib dihydrochloride

描述: Veliparib dihydrochloride (ABT-888 dihydrochloride) 是一种PARP1和PARP2抑制剂，Ki 分别为5.2 nM 和2.9 nM。

激酶实验: PARP assays are conducted in a buffer containing 50 mM Tris (pH 8.0), 1 mM DTT, 1.5 μM [3H]NAD+?(1.6 μCi/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.

体外活性: Veliparib is inactive to SIRT2 (>5 μM)[1]. Veliparib inhibits the PARP activity with EC50 of 2 nM in C41 cells[2]. Veliparib can decrease the PAR levels in both irradiated and nonirradiated H460 cells. Veliparib reduces clonogenic survival and inhibits DNA repair by PARP-1 inhibition in H460 cells. Veliparib increases apoptosis and autophagy in H460 cells when combined with radiation[3]. Veliparib inhibits PARP activity in H1299, DU145 and 22RV1 cells and the inhibition is independent of p53 function. Veliparib (10 μM) suppresses the surviving fraction (SF) by 43% in the clonogenic H1299 cells. Veliparib exhibits effective radiosensitivity in oxic H1299 cells. Veliparib can attenuate the SF of hypoxic-irradiated cells including H1299, DU145 and 22RV1[4].

体内活性: The oral bioavailability of Veliparib is 56%-92% in mice, SD rats, beagle dogs, and cynomolgus monkeys after oral administration[1]. Veliparib (25 mg/kg, i.p.) can improve tumor growth delay in a NCI-H460 xenograft model. Veliparib decreases tumor vessel formation when combine with radiation[3]. Veliparib 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 can be maintained over time[4].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 3.2 mg/mL (10.09 mM)
H2O : 50 mg/mL (157.62 mM)


关键字: Autophagy | Veliparib | poly ADP ribose polymerase | ABT 888 Dihydrochloride | ABT888 | inhibit | Veliparib dihydrochloride | ABT-888 Dihydrochloride | Inhibitor | ABT-888 | Veliparib Dihydrochloride | ABT888 Dihydrochloride | ABT 888 | PARP

相关产品: Excisanin A | Rubiadin | Euchrestaflavanone B | G007-LK | PJ34 hydrochloride | PARP-1/2-IN-2 | G244-LM | Niraparib (R-enantiomer) | Dehydrocorydaline nitrate | ARTD10/PARP10-IN-1

相关库: Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | Anti-Cancer Compound Library | Anti-Cancer Drug Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Active Compound Library | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library