ETP-46464|cas:1345675-02-6|西域试剂

ETP-46464,99.55%

产品编号：Bellancom-15521| CAS NO：1345675-02-6| 分子式：C₃₀H₂₂N₄O₂| 分子量：470.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-15521	￥900.00	杭州北京（现货）
Bellancom-15521	￥1400.00	杭州北京（现货）
Bellancom-15521	￥5000.00	杭州北京（现货）
Bellancom-15521	￥9000.00	杭州北京（现货）

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ETP-46464

产品介绍

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 IC₅₀s of 0.6 and 14 nM, respectively.

体外研究

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 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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

性状

Solid

溶解性数据

In Vitro:

DMSO : 5 mg/mL (10.63 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1253 mL	10.6265 mL	21.2531 mL
5 mM	0.4251 mL	2.1253 mL	4.2506 mL
10 mM	0.2125 mL	1.0627 mL	2.1253 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.5 mg/mL (1.06 mM); Clear solution

此方案可获得 ≥ 0.5 mg/mL (1.06 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 5.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液