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AZ32

Cat. No. M10158
AZ32 Structure
Synonym:

AZ-32

Size Price Availability
10mg USD 285  USD285 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZ32 blocks the DNA damage response and radiosensitized GBM cells in vitro. AZ32 is highly efficient in vivo as radiosensitizer in syngeneic and human, orthotopic mouse glioma model compared with AZ31. Following a single oral dose of AZ32 (200 mg/kg) in mice, the free-brain concentrations of AZ32 are in excess of the cellular IC50 for approximately 22 hours.

Protocol
Cell Experiment
Cell lines U1242 cells
Preparation method Human glioma U1242 cells were treated with AZ32 (3 μM) and radiation (2 Gy) or left untreated. At 48 hrs the cells were fixed and processed for ICC using anti-γ-tubulin (centrosomes) and -α-tubulin (microtubules). Cells were counterstained with DAPI to visualize nuclei.
Concentrations 3 μM
Incubation time 48 h
Animal Experiment
Animal models orthotopic GL261 glioma model (GL261/luc-red cells intracranially injected into C57bl6 mice)
Formulation in hydroxypropyl-methyl cellulose (0.5%w/v)/0.1%w/v polysorbate-80 to 20 mg/ml
Dosages 200 mg/kg
Administration oral gavage
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 328.37
Formula C20H16N4O
CAS Number 2288709-96-4
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

[1] Jeremy Karlin, et al. Mol Cancer Ther. Orally Bioavailable and Blood-Brain Barrier-Penetrating ATM Inhibitor (AZ32) Radiosensitizes Intracranial Gliomas in Mice

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZ32, AZ-32 supplier, ATM/ATR, inhibitors

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