ETP-46464 是一种有效的 mTOR 和 ATR 抑制剂，IC₅₀ 分别为 0.6 和 14 nM。

ETP-46464 is an effective mTOR and ATR inhibitor with IC 50 s of 0.6 and 14 nM, respectively.

Solid

mTOR 0.6 nM (IC50) ATR 14 nM (IC50

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 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 LD50 range 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 activit

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Toledo LI, et al. A cell-based screen identifies ATR inhibitors with synthetic lethal properties for cancer-associated mutations. Nat Struct Mol Biol. 2011 Jun;18(6):721-7.
[2]. Teng PN, et al. Pharmacologic inhibition of ATR and ATM offers clinically important distinctions to enhancing platinum or radiation response in ovarian, endometrial, and cervical cancer cells. Gynecol Oncol. 2015 Mar;136(3):554-61.

In Vitro: DMSO : 5 mg/mL (10.63 mM; Need ultrasonic)配制储备液