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AZ20

Cat. No. M2412
AZ20 Structure
Size Price Availability Quantity
5mg USD 60  USD60 In stock
10mg USD 90  USD90 In stock
25mg USD 180  USD180 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AZ20 is a novel potent and selective inhibitor of ATR kinase with IC50 of 5 nM, 8-fold selectivity over mTOR. In vitro, AZ20 decreases pChk1 Ser345, pChk1 Ser317 and pChk1 Ser296 levels in a concentration-dependent manner. Prolonged exposure with AZ20 increases  H2AX pan-nuclear staining, indicative of replication stress. AZ20 induces growth inhibition and cell death and its profile of activity is distinctly when compares with other cytotoxic agents. in vivo,AZ20 induces significant tumour growth inhibition at well tolerated doses.

Product Citations
Customer Product Validations & Biological Datas
Source Sci Rep (2017). Figure 1. AZ20
Method flow cytometry analyses
Cell Lines AML cell lines
Concentrations 0–8 μM
Incubation Time 24 h
Results Based on the samples tested, AZ20 sensitivity appeared to be similar between these two groups (p = 0.8, calculated using the Mann-Whitney U-test).
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 412.51
Formula C21H24N4O3S
CAS Number 1233339-22-4
Purity >98%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

[1] Foote KM, et al. J Med Chem. Abstract 1823: AZ20, a novel potent and selective inhibitor of ATR kinase with in vivo antitumour activity.

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  Catalog
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