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ETP-46464

Cat. No. M2187
ETP-46464 Structure
Size Price Availability Quantity
5mg USD 85  USD85 In stock
10mg USD 130  USD130 In stock
50mg USD 480  USD480 In stock
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Quality Control & Documentation
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.

Customer Product Validations & Biological Datas
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.
Protocol (for reference only)
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
Chemical Information
Molecular Weight 470.52
Formula C30H22N4O2
CAS Number 1345675-02-6
Solubility (25°C) DMSO 6 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Choi S, et al. DNA Repair (Amst). CGK733 does not inhibit ATM or ATR kinase activity in H460 human lung cancer cells.

[2] Toledo LI, et al. Nat Struct Mol Biol. A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations.

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


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