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ETP-46464

Cat. No. M2187
ETP-46464 Structure
Size Price Availability Quantity
10mg USD 160 In stock
50mg USD 650 In stock
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Quality Control
Biological Activity

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.

Protocol
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
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 470.52
Formula C30H22N4O2
CAS Number 1345675-02-6
Purity 100.00%
Solubility DMSO 10 mg/mL
Storage at -20°C
References

CGK733 does not inhibit ATM or ATR kinase activity in H460 human lung cancer cells.
Choi S, et al. DNA Repair (Amst). 2011 Oct 10;10(10):1000-2. PMID: 21865098.

A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.
Toledo LI, et al. Nat Struct Mol Biol. 2011 Jun;18(6):721-7. PMID: 21552262.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: ETP-46464 supplier, ATM/ATR, inhibitors

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