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AZD1390

Cat. No. M9581
AZD1390 Structure
Synonym:

AZD-1390

Size Price Availability Quantity
5mg USD 197  USD197 In stock
10mg USD 310  USD310 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD1390 is a potent and selective inhibitor of ATM in cells (IC50 = 0.78 nM) with the ability to cross the blood-brain barrier. AZD1390 has >10,000-fold selectivity over closely related members of the PIKK family of enzymes and excellent selectivity across a broad panel of kinases. AZD1390 displays excellent oral bioavailability in preclinical species (66% in rat and 74% in dog), is not a substrate for human efflux transporters, and has been shown to efficiently cross the BBB in non-human primate PET studies.

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 477.57
Formula C27H32FN5O2
CAS Number 2089288-03-7
Purity >99%
Solubility DMSO ≥ 15 mg/mL (May need warming)
Storage at -20°C
References

[1] Stephen T Durant, et al. Sci Adv. The Brain-Penetrant Clinical ATM Inhibitor AZD1390 Radiosensitizes and Improves Survival of Preclinical Brain Tumor Models

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD1390, AZD-1390 supplier, ATM/ATR, inhibitors

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