[CAS NO. 2088113-98-6] AZ31
PRODUCTS SPECIFICATIONS [2088113-98-6]
DESCRIPTION [2088113-98-6]
Overview
| MDL | MFCD31922712 |
|---|---|
| Molecular Weight | 420.50 |
| Molecular Formula | C24H28N4O3 |
| SMILES | O=C(C1=C(N[C@@H](C)C2CCOCC2)C3=CC(C4=CC=C(COC)N=C4)=CC=C3N=C1)N |
Summary
AZ31 is a a potent, highly selective, and orally active ATM inhibitor with an IC 50 of <1.2 nM for ATM enzyme, and an IC 50 of 46 nM for ATM in cell. AZ31 shows excellent selectivity over ATR (>500-fold) and excellent PIKK-family selectivity and pan-kinase selectivity. AZ31 is a potent radiosensitizer in vitro, it can be used for the research of cancer [1] .
IC50 & Target
|
ATM 1.2 nM (IC 50 ) |
ATM 46 nM (IC 50 , in cell) |
In Vitro
AZ31 (0.3-3 μM; 1 h) affects phosphorylation of a panel of ATM targets
[1]
.
AZ31 (10 μM; 1 h) affects stabilization of p53 in H2228 lung cancer cells after radiation
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | Human glioma cell line |
| Concentration: | 0.3, 1 and 3 μM |
| Incubation Time: | 1 hour |
| Result: | Blocked phosphorylation of p53-S15, KAP1-S824, and ATM auto-phosphorylation at S1981. |
Western Blot Analysis [1]
| Cell Line: | H460 and mutant p53 H2228 cell lines |
| Concentration: | 10 μM |
| Incubation Time: | 1 hour |
| Result: | Destabilized p53 of mutant p53 but not wild-type after radiation. |
In Vivo
AZ31 (50-100 mg/kg; p.o. twice a day) shows low brain coverage [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Nude mice [1] |
| Dosage: | 50 and 100 mg/kg |
| Administration: | Oral gavage; 50 and 100 mg/kg twice a day |
| Result: | Exhibited exposure over IC 50 at 0.046 μM in brain only for 2-3 hours. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
