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Chemical Structure| 1345675-02-6 Chemical Structure| 1345675-02-6

Structure of ETP-46464
CAS No.: 1345675-02-6

Chemical Structure| 1345675-02-6

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ETP-46464 is a cell-permeable quinoline-containing heterotricyclic compound that acts as a potent inhibitor against mTOR, ATR, DNA-PK, PI 3-Kα, and ATM (IC50= 0.6, 14, 36, 170, and 545 nM, respectively).

Synonyms: ATM Inhibitor III; ATR Inhibitor III

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Product Details of ETP-46464

CAS No. :1345675-02-6
Formula : C30H22N4O2
M.W : 470.52
SMILES Code : N#CC(C)(C)C1=CC=C(N(C2=C3C=NC4=CC=C(C5=CC6=CC=CC=C6N=C5)C=C24)C(OC3)=O)C=C1
Synonyms :
ATM Inhibitor III; ATR Inhibitor III
MDL No. :MFCD23160051

Safety of ETP-46464

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of ETP-46464

DNA
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTOR

    mTOR, IC50:0.6 nM

  • ATM

    ATM, IC50:545 nM

  • ATR

    ATR, IC50:14 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
3T3TopBP1-ER cells 10 μM 15 minutes To screen for ATR inhibitors by detecting ATR activity through 4-OHT-induced γH2AX signal. PMC4869831
U2OS cells 1 μM 4 hours To evaluate the ability of the compounds to inhibit ATR upon exposure to ionizing radiation (IR), results showed that the compounds could abrogate the G2/M checkpoint. PMC4869831
BJ/TERT LT cells 4 µM 24 hours ATR kinase inhibition led to a dose dependent decrease in OASL and IRF1 protein expression PMC4078001
BJ/TERT LT cells 5 µM 3 hours ATR kinase inhibition decreased the LT protection of cells from virus mediated cell death PMC4078001
A2780 5 µM 72 hours To evaluate the effect of ETP-46464 on cisplatin sensitivity, results showed that ETP-46464 significantly enhanced the cell-killing effect of cisplatin. PMC4382918
OVCAR3 5 µM 72 hours To evaluate the effect of ETP-46464 on cisplatin sensitivity, results showed that ETP-46464 significantly enhanced the cell-killing effect of cisplatin. PMC4382918
HELA 5 µM 72 hours To evaluate the effect of ETP-46464 on cisplatin sensitivity, results showed that ETP-46464 significantly enhanced the cell-killing effect of cisplatin. PMC4382918
HEC1B 5 µM 72 hours To evaluate the effect of ETP-46464 on cisplatin sensitivity, results showed that ETP-46464 significantly enhanced the cell-killing effect of cisplatin. PMC4382918
lung cancer cell lines 10 μM 4 hours To observe the effect of ATR kinase inhibitor ETP-46464 on lung cancer cell lines, results showed that ETP-46464 disrupted gemcitabine-induced Chk1 serine 345 phosphorylation. PMC4595318
PD5 mouse ovarian cells 1 μM 96 hours To investigate the effect of 4-HC on primordial follicles, confirming that 4-HC induces primordial oocyte death through activation of apoptotic pathways PMC6540791
HEK293T cells 2 μM 6 hours To investigate the effect of ETP-46464 on the interaction between ATAD5 and RAD51, results showed that ETP-46464 inhibited the HU-induced interaction between ATAD5 and RAD51. PMC6914801

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice PD5 mice intraperitoneal injection 20 μM Single injection To investigate the effect of CPA on primordial follicles, confirming that CPA induces primordial oocyte death through activation of apoptotic pathways PMC6540791

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.63mL

2.13mL

1.06mL

21.25mL

4.25mL

2.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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