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AZ31

Cat. No. M9128
AZ31 Structure
Synonym:

AZ-31

Size Price Availability
5mg USD 147  USD147 Custom Synthesis
10mg USD 250  USD250 Custom Synthesis
50mg USD 810  USD810 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

AZ31 is a potent and highly selective ATM inhibitor with an IC50 of <0.0012 μM. AZ31 is the first selective orally active and bioavailable ATM kinase inhibitor.

In vivo, pharmacokinetic investigation of AZ31 as a single agent and in combination with irinotecan revealed that plasma concentrations of AZ31 were highest 1-hour after administration followed by a stepwise decrease at 3, 6 and 16 hour in the combination sensitive CRC098.

Protocol
Cell Experiment
Cell lines CRC (metastatic colorectal cancer) cell lines: HCT15, HCT116, RKO, CaCo2, LS123 and LOVO
Preparation method Six CRC cell lines were treated with AZ31 (dose 1.25, 2.5 or 5 μmol/L), SN38 (0.3125 -20 nM) or AZ31 + SN38 and proliferation was determined by an SRB assay.
Concentrations 1.25, 2.5 or 5 μmol/L
Incubation time 72 hours
Animal Experiment
Animal models CRC PDX models (Four-to-six week-old female athymic nude mice with implanted patient-derived colorectal adenocarcinoma tumor)
Formulation 10% v/v DMSO + 90% v/v Captisol at 30% w/v
Dosages 100 mg/kg-daily × 3
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 420.50
Formula C24H28N4O3
CAS Number 2088113-98-6
Purity >98%
Solubility DMSO: ≥ 40 mg/mL
Storage at -20°C
References

[1] Greene J, et al. Oncotarget. The novel ATM inhibitor (AZ31) enhances antitumor activity in patient derived xenografts that are resistant to irinotecan monotherapy.

[2] Kiesel BF, et al. J Pharm Biomed Anal. LC-MS/MS assay for the simultaneous quantitation of the ATM inhibitor AZ31 and the ATR inhibitor AZD6738 in mouse plasma.

[3] Degorce SL, et al. J Med Chem. Discovery of Novel 3-Quinoline Carboxamides as Potent, Selective, and Orally Bioavailable Inhibitors of Ataxia Telangiectasia Mutated (ATM) Kinase.

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RP-3500

RP-3500 (ATR inhibitor 4) is an orally potent, selective ATR kinase inhibitor (ATRi) in biochemical assays IC50 1.00 nM. The RP-3500 is 30 times more selective to ATR (IC).50=120 nM), which is 2,000 times > ATM, DNA-PK, and PI3Kα kinase.

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  Catalog
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Keywords: AZ31, AZ-31 supplier, ATM/ATR, inhibitors

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