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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.
| 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 |
| Molecular Weight | 420.50 |
| Formula | C24H28N4O3 |
| CAS Number | 2088113-98-6 |
| Solubility (25°C) | DMSO: ≥ 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related ATM/ATR Products |
|---|
| KU-55933
KU-55933 is a cell-permeable ATP-competitive inhibitor of ATM (IC50 = 13 nM; Ki = 2.2 nM) with selectivity over other PIKK family kinases (IC50 = 2.5, 9.3, 16.6 μM for DNAPK, mTOR, PI 3-K, respectively; IC50 > 100 μM for PI 4-K and ATR). |
| KU-60019
KU-60019 is a potent ATM kinase inhibitor with IC50 of 6.3 nM. |
| VE-821
VE-821 is a highly selective and potent ATR inhibitor with IC50 of 26 nM. |
| ETP-46464
ETP-46464 is a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα and ATM with IC50 of 0.6, 14, 36, 170 and 545 nM, respectively. |
| CP-466722
Cp-466722 is a reversible ATM inhibitor with IC50 value of 4.1 μM, but has no effect on PI3K, PIKK family proteins. |
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