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ETP-46464
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ETP-46464
CAS No. : 1345675-02-6
MCE 站:ETP-46464
产品活性:ETP-46464 是一种有效的 mTOR 和 ATR 抑制剂,IC50 分别为 0.6 和 14 nM。
研究领域:PI3K/Akt/mTOR | Cell Cycle/DNA Damage
In Vitro: ETP-46464 (ATRi) also inhibits DNA-PK, PI3Kα and ATM with IC50s of 36 nM, 170 nM and 545 nM, respectively. Platinum-sensitive and -resistant ovarian, endometrial and cervical cancer cell lines are treated with varying levels of Cisplatin (0-50 ?M) with or without the ETP-46464 (5.0 ?M) and/or the KU55933 (10.0 ?M) for 72 h. Single-agent dose response analyses of ETP-46464 and KU55933 in a subset of cell lines reveal a wide LD50 range of 10.0±8.7 and 38.3±7.6 ?M respectively. Co-treatment doses are chosen based on these studies and previously published evidence of phospho-Chk1 (Ser345) and phospho-ATM (Ser1981) inhibition following ionizing radiation exposure and dose response treatments with ETP-46464 and KU55933. Treatment with ETP-46464 significantly increases the response of Cisplatin in all cell lines tested, resulting in 52-89% enhancement in activity and are synergistic. The combined inhibition of ATR and ATM enhances the response of Cisplatin to a level equivalent to that observed using ETP-46464 alone. These effects are independent of p53 status, and are observed in all gynecologic (GYN) cancer cells tested. Treatment with ETP-46464, but not KU55933, not only sensitizes these GYN cancer cell lines to Cisplatin, but also enhances the response of Carboplatin.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Kinase Inhibitor Library | PI3K/Akt/mTOR Compound Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Autophagy Compound Library | Anti-Aging Compound Library | Antioxidants Compound Library | Differentiation Inducing Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Glycolysis Compound Library | Cytoskeleton Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Rapamycin | Everolimus | MHY1485 | 3BDO | Temsirolimus | Salidroside | Torkinib | PI-103 | D-α-Hydroxyglutaric acid disodium | L-Leucine | AZ20 | Dihydromyricetin | CGK733 | PKI-402 | Polyphyllin I | Rheb inhibitor NR1 | GSK1059615 | GNE-317 | AZ32 | PP121 | CP-466722 | WYE-354 | Cyclovirobuxine D | HDACs/mTOR Inhibitor 1 | XL388 | Palomid 529 | WAY-600 | Arnicolide D | (+)-Usnic acid | Garci C
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