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A-966492

Cat. No. M3410

A-966492 Structure
Size Price Availability Quantity
5mg USD 130 In stock
10mg USD 220 In stock
50mg USD 700 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

A-966492 is a highly potent and efficacious poly (ADP-ribose) polymerase (PARP) inhibitor with a Ki and EC50 of 1 nM. In addition, it is orally bioavailable across multiple species, crosses the blood-brain barrier, and appears to distribute into tumor tissue. It also demonstrated good in vivo efficacy in a B16F10 subcutaneous murine melanoma model in combination with temozolomide and in an MX-1 breast cancer xenograft model both as a single agent and in combination with carboplatin.

Protocol
Cell Experiment
Cell lines C41 cell
Preparation method Treating C41 cells with A-966492 for 30 minutes in a 96-well plate . Activating PARP by damaging DNA with 1 mM H2O2 for 10 minutes. Washing cells with ice-cold phosphate-buffered saline (PBS) once and fixing with prechilled methanol/acetone (7:3) at -20 °C for 10 minutes. When they are air-dried, rehydrating plates with PBS and blocked using 5% nonfat dry milk in PBS-Tween(0.05%) (blocking solution) for 30 minutes at room temperature. Incubating cell with anti-PAR antibody 10H (1:50) in blocking solution at room temperature for 60 minutes followed by washing with PBS-Tween20 five times, and incubation with goat antimouse fluorescein 5(6)-isothiocyanate (FITC)-coupled antibody (1:50) and 1 μg/mL 40,6-diamidino-2-phenylindole (DAPI) in blocking solution at room temperature for 60 minutes. After washing with PBS-Tween20 5 times, using an fmax Fluorescence Microplate Reader set at the excitation and emission wavelength for FITC or the excitation and emission wavelength for DAPI to perform analysis. Normalizing PARP activity (FITC signal) with cell numbers (DAPI).
Concentrations ~10 nM
Incubation time 30 minutes
Animal Experiment
Animal models A 0.2 cc amount of a 1:10 dilution of tumor brei in 45% Matrigel and 45% Spinner MEM is injected subcutaneously into the flank of female SCID mice.
Formulation
Dosages 12.5, 25, and 50 mg/kg/day, for 14 days
Administration Orally administrated
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 324.35
Formula C18H17FN4O
CAS Number 934162-61-5
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
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BMN673 isomer

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: A-966492 supplier, PARP, inhibitors

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