Veliparib [912444-00-9]

Catalog number: HY-10129_200mg
Brand: MedChem Express
Packing: 200 mg
Other sizes: 5 mg
10 mM
10 mg
50 mg
100 mg
Price: € 637.00
Expected delivery time: 10 days

Product specifications for - Veliparib [912444-00-9]

Product group: Chemicals
Category: Inhibitors / activators
CAS No.: 912444-00-9
Purity: >98%
Molecular Formula: C13H16N4O
Molecular weight: 244,2923
Datasheet: Datasheet
  Research Use Only
UNSPSC: 12352200
Scientific information: 
Scientific info: Veliparib is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively. IC50 & Target: Ki: 5.2 nM (PARP1), 2.9 nM (PARP2)[1] 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 uM. 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 uM, respectively[1]. 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 uM Veliparib (ABT-888). When treated with 38 uM 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[2]. In HaCaT cells, at 6 h post-treatment by Veliparib (ABT-888), cell viability is significantly increases under 1,000 uM sulfur mustard (SM) exposure, whereas Veliparib does not protect cell viability under 100 uM SM exposure. Moreover, the addition of Veliparib no longer shows the protective effect at 24 h post SM exposure[3]. In Vivo: Veliparib (ABT-888) is a potent inhibitor of PARP, has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models[1]. In MDA-MB-231 xenograft tumor models, combination treatment (AG014699/Crizotinib and Veliparib (ABT-888)/Foretinib) substantially reduced tumor growth compared to either inhibitor alone[2].
Safety information: 
Additional information: 
Synonyms: HY-10129