All AbMole products are for research use only, cannot be used for human consumption.
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. ETP-46464 preferentially suppresses radiation-induced cellular ATR activity (>90% at 500 nM) over ATM or DNA-PK activity (IC50 > 5 μM) in U2OS cells, while exhibiting much reduced or little potency toward a panel of 26 other kinases (>55% inhibition at 5 μM). ETP-46464 (10 μM) inhibited the UV-induced phosphorylation of CHK1 serine 317. Further, the phosphorylation of ATM serine 1981 was increased in cells incubated in 10 μM ETP-46464 and exposed to 10 J/m2 UV.
 |
Source | Gynecol Oncol (2015). Figure 3. ETP-46464 |
| Method | Immunoblot | |
| Cell Lines | Gynecologic carcinoma cells | |
| Concentrations | 5 μM | |
| Incubation Time | 3 h | |
| Results | The GYN cancer cell lines were treated at their respective LD50 levels of cisplatin alone or in combination with ATRi (5.0 μM ETP-46464) and/or ATMi (10.0 μM KU55933) for 3 h. Total ATR, ATM, Chk1 and Chk2 did not vary significantly under any of these treatment conditions. |
| Cell Experiment | |
|---|---|
| Cell lines | 23T, 239T, Calu6 and H460 cells line |
| Preparation method | Proliferation assays MTT Assay (Trevigen, Gaithersburg, MD) was used to measure cell proliferation. Drug combinations were evaluated using CalcuSyn (BIOSOFT, Ferguson, MO) software based on the multiple drug effect equation of Chou-Talalay. Experimental values were imputed into Calcusyn to calculate IC50 and a combination index (CI, a quantitative measure of the synergy (CI < 1), additivity (CI = 1), or antagonism (CI > 1) between drugs). Log-transformed CI’s are plotted against growth inhibition/effective dose (ED) with corresponding 95 % confidence intervals. Synergism is indicated when the 95 % CI falls below the x-axis (log CI = 0; CI = 1), whereas antagonism is indicated when the 95 % CI falls above the x-axis, at each respective region of the effective dose. |
| Concentrations | |
| Incubation time | 2 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 470.52 |
| Formula | C30H22N4O2 |
| CAS Number | 1345675-02-6 |
| Solubility (25°C) | DMSO 5 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.
