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ETP-46464

目录号: PL04452 纯度: ≥99%

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

CAS No. :1345675-02-6

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中文名称	ETP-46464
中文别名	ALPHA,ALPHA-二甲基-4-[2-氧代-9-(3-喹啉基)-2H-[1,3]恶嗪并[5,4-C]喹啉-1(4H)-基]-苯乙腈;ETP46464 抑制剂;腺苷-5′-二磷酸;alpha,alpha-二甲基-4-[2-氧代-9-(3-喹啉基)-2H-[1,3]恶嗪并[5,4-c]喹啉-1(4H)-基]-苯乙腈
英文名称	ETP-46464
英文别名	ETP-46464;2-Methyl-2-(4-(2-oxo-9-(quinolin-3-yl)-2,4-dihydro-1H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl)propanenitrile;2-methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile;ETP46464;4-[4-(1-Isocyano-1-methyl-ethyl)-phenyl]-6-quinolin-3-yl-1,4-dihydro-2-oxa-4,9-diaza-phenanthren-3-one;ATRi;2-Methyl-2-[4-(2-oxo-9-quinolin-3-yl-4H-[1,3]oxazino[5,4-c]quinolin-1-yl)phenyl]propanenitrile
Cas No.	1345675-02-6
分子式	C₃₀H₂₂N₄O₂
分子量	470.52
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	ETP-46464 是一种有效的 mTOR 和 ATR 抑制剂，IC50 分别为 0.6 和 14 nM。

产品详情	ETP-46464 是一种有效的 mTOR 和 ATR 抑制剂，IC₅₀ 分别为 0.6 和 14 nM。
生物活性	ETP-46464 is an effective mTOR and ATR inhibitor with IC 50 s of 0.6 and 14 nM, respectively.
性状	Solid
IC50 & Target[1][2]	mTOR 0.6 nM (IC50) ATR 14 nM (IC50
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. 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
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[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.

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

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[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.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

ETP-46464

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