All AbMole products are for research use only, cannot be used for human consumption.
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 |
|---|
| ART0380
ART0380 is a potent and selective ATR kinase inhibitor. |
| KU 59403
KU 59403 is a potent ATM inhibitor, with IC50 values of 3 nM, 9.1 μM and 10 μM for ATM, DNA-PK and PI3K, respectively. |
| SKLB-197
SKLB-197 showed an IC50 value of 0.013 μM against ATR but very weak or no activity against other 402 protein kinases. |
| ATR-IN-4
ATR-IN-4 is a potent ATR (Ataxia telangiectasia mutated gene Rad 3-associated kinase) inhibitor. |
| M3541
M3541 is a potent, ATP-competitive and selective ATM inhibitor with an IC50 of 0.25 nM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
