CAS NO: | 1345675-02-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | ETP-46464 is an effectivemTORandATRinhibitor withIC50s of 0.6 and 14 nM, respectively. | ||||||||||||||||
IC50& Target[1] |
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体外研究 (In Vitro) | ETP-46464 (ATRi) also inhibits DNA-PK, PI3Kα and ATM with IC50s of 36 nM, 170 nM and 545 nM, respectively[1]. Platinum-sensitive and -resistant ovarian, endometrial and cervical cancer cell lines are treated with varying levels of Cisplatin (0-50 μM) with or without the ETP-46464 (5.0 μM) and/or the KU55933 (10.0 μM) for 72 h. Single-agent dose response analyses of ETP-46464 and KU55933 in a subset of cell lines reveal a wide LD50range of 10.0±8.7 and 38.3±7.6 μM 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[2]. | ||||||||||||||||
分子量 | 470.52 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C30H22N4O2 | ||||||||||||||||
CAS 号 | 1345675-02-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 5 mg/mL(10.63 mM;Need ultrasonic) 配制储备液
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