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Veliparib
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Veliparib
CAS No. : 912444-00-9
MCE 站:Veliparib
产品活性:Veliparib (ABT-888) 是一种有效的 PARP 抑制剂,抑制 PARP1 和 PARP2 的 Ki 分别为 5.2 和 2.9 nM。
研究领域:Cell Cycle/DNA Damage | Epigenetics | Autophagy
In Vitro: Veliparib (ABT-888) is also tested against SIRT2, an enzyme that also uses NAD+ for catalysis, and found to be inactive (>5,000 nM). The receptor profile of Veliparib is determined in a panel of 74 receptor-binding assays at a concentration of 10 μM. Veliparib displaces control-specific binding at 50% or greater at the human H1(61%), the human 5-HT1A (91%), and the human 5-HT7 (84%) sites only. The IC50s for these three receptors are 5.3, 1.5, and 1.2 μM, respectively. c-Met knockdown cells show 4.2- (shMet-A; 95% CI=4-4.5) or 4.6-fold (shMet-B; 95% CI=4.4-4.8) growth inhibition when treated with 60 μM Veliparib (ABT-888). When treated with 38 μM Veliparib, c-Met knockdown cells show 2- (shMet-A; 95% CI=1.5-2.5) or 1.9-fold (shMet-B; 95% CI=1.3-2.5) growth inhibition. In HaCaT cells, at 6 h post-treatment by Veliparib (ABT-888), cell viability is significantly increases under 1,000 ?M sulfur mustard (SM) exposure, whereas Veliparib does not protect cell viability under 100 ?M SM exposure. Moreover, the addition of Veliparib no longer shows the protective effect at 24 h post SM exposure.
In Vivo: Veliparib (ABT-888) is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier in syngeneic and xenograft tumor models. In MDA-MB-231 xenograft tumor models, combination treatment (AG014699/PF-02341066 and Veliparib (ABT-888)/Foretinib) substantially reduced tumor growth compared to either inhibitor alone.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | CNS-Penetrant Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Drug Repurposing Compound Library | Anti-COVID-19 Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | XAV-939 | Rucaparib | PJ34 | 3-Aminobenzamide | G007-LK | Dehydrocorydaline chloride | AG14361 | Iniparib | AZD-2461 | BGP-15 | Fucosterol | JW 55 | EB-47 dihydrochloride | UPF 1069 | AZ6102 | iRucaparib-AP6 | ME0328 | MN-64 | 5,?7,?4'-?Trimethoxyflavone | Benzamide | GeA-69 | Paris saponin VII | PARP14 inhibitor H10 | BYK204165 | NU1025 | Oroxin A
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热门标签:ABT-888