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ABT-888

Cat. No. M1639

ABT-888 Structure

Synonym: Veliparib

Size Price Availability Quantity
10mg USD 85 In stock
50mg USD 280 In stock
200mg USD 600 In stock
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Quality Control
Biological Activity

ABT-888 (Veliparib) is a potent inhibitor of PARP-1 and PARP-2 with Ki values of 5.2nM and 2.9nM respectively. ABT-888 (Veliparib) inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. ABT-888 (Veliparib) has good oral bioavailability, can cross the blood-brain barrier, and potentiates temozolomide, platinums, cyclophosphamide, and radiation in syngeneic and xenograft tumor models. This broad spectrum of chemopotentiation and radiopotentiation makes this compound an attractive candidate for clinical evaluation. Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults reveal that PARP inhibition can modulate the capacity to repair topoisomerase I-mediated DNA damage in the clinic.

Protocol
Cell Experiment
Cell lines C41 cells
Preparation method Cellular PARP Assay. C41 cells were treated with test compound for 30 min in a 96-well plate. PARP was activated by damaging DNA with 1 mM H2O2 for 10 min. Cells were washed with ice-cold PBS once and fixed with prechilled methanol/acetone (7:3) at -20 °C for 10 min. After air-drying, plates were rehydrated with PBS and blocked using 5% nonfat dry milk in PBS-tween (0.05%) (blocking solution) for 30 min at room temperature. Cells were incubated with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 min followed by washing with PBS-Tween20 5 times and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 µg/mL 4′,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 min. After washing with PBS-Tween20 5 times, analysis was performed using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI. PARP activity (FITC signal) was normalized with cell numbers (DAPI).
Concentrations 0~1uM
Incubation time 30 min
Animal Experiment
Animal models MX-1 Tumor Model
Formulation 2.5% EtOH, 1 drop TW-80, 25% PEG400, PBS
Dosages 12.5mg/kg, BID, P6-11
Administration orally
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 244.29
Formula C13H16N4O
CAS Number 912444-00-9
Purity 100%
Solubility DMSO ≥45 mg/mL
Storage at -20°C
References

Phase I study of PARP inhibitor ABT-888 in combination with topotecan in adults with refractory solid tumors and lymphomas.
Kummar et al. Cancer Res. 2011 Sep 1;71(17):5626-34. PMID: 21795476.

The poly(ADP-Ribose) polymerase inhibitor ABT-888 reduces radiation-induced nuclear EGFR and augments head and neck tumor response to radiotherapy.
Nowsheen et al. Radiother Oncol. 2011 Jun;99(3):331-8. PMID: 21719137.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ABT-888, Veliparib supplier, PARP, inhibitors

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