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PI3K/Akt/mTOR 肿瘤表观遗传和基因调控
/ ATM/ATR / Elimusertib

Elimusertib {[allProObj[0].p_purity_real_show]}

货号：A164508 同义名： BAY-1895344

BAY-1895344 is a potent and selective ATR inhibitor with IC50 of 7 nM.

Elimusertib 化学结构 CAS号：1876467-74-1
Elimusertib 化学结构
CAS号：1876467-74-1
Elimusertib 3D分子结构
CAS号：1876467-74-1
Elimusertib 化学结构 CAS号：1876467-74-1
Elimusertib 3D分子结构 CAS号：1876467-74-1
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Elimusertib 纯度/质量文件 产品仅供科研

货号：A164508 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ATM ↓ ATR ↓ 其他靶点 纯度
Wortmannin ++

ATM, IC50: 150 nM

 		PI3K,DNA-PK,MLCK 99%+
CP-466722 +

ATM, IC50: 410 nM

 		99%+
Torin 2 ++

ATM, EC50: 28 nM

 		++

ATR, EC50: 35 nM

 		mTOR,DNA-PK 99%+
KU-55933 +++

ATM, IC50: 12.9 nM

 		96%
ETP-46464 +

ATM, IC50: 545 nM

 		+++

ATR, IC50: 14 nM

 		mTOR,DNA-PK 98%
CGK733 ++

ATM, IC50: 200 nM

 		++

ATR, IC50: 200 nM

 		99%+
AZD0156 ✔ 99%+
Dactolisib +++

ATR, IC50: 21 nM

 		98+%
Ceralasertib ++++

ATR, IC50: 1 nM

 		99%+
Berzosertib +++

ATR, IC50: 19 nM

 		99%+
VE-821 +++

ATR, Ki: 13 nM

 		99%+
AZ20 ++++

ATR, IC50: 5 nM

 		mTOR 99%+
Schizandrin B +

ATR, IC50: 7.25 μM

 		P-gp 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Elimusertib 生物活性

描述 Elimusertib, also known as BAY-1895344, is an effective, orally active, selective ATR inhibitor with an IC50 of 7 nM. It exhibits antitumor activity[1][2]. Elimusertib effectively inhibits the proliferation of various human tumor cell lines, with a median IC50 value of 78 nM. Elimusertib also effectively inhibits hydroxyurea-induced H2AX phosphorylation (IC50: 36 nM)[1]. Elimusertib exhibits effective anti-proliferative activity in vitro against various cancer cell lines, such as in the CRC cell lines HT-29 (IC50: 160 nM) and LoVo (IC50: 71 nM), as well as in the B-cell lymphoma cell line SU-DHL-8 (IC50: 9 nM)[3].

Elimusertib 动物研究

Animal study Elimusertib demonstrates effective antitumor efficacy as a monotherapy in various ovarian and colorectal cancer xenograft models, and leads to complete remission of tumors in mantle cell lymphoma models[2].

Elimusertib 参考文献

[1]Ulrich T. Luecking, et al. Abstract 983: Identification of potent, highly selective and orally available ATR inhibitor BAY 1895344 with favorable PK properties and promising efficacy in monotherapy and combination in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement.

[2]Antje Margret Wengner, et al. Abstract 836: ATR inhibitor BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride in preclinical tumor models. Cancer Research. July 2017 Volume 77, Issue 13 Supplement

[3]Ulrich Lücking, et al. Damage Incorporated: Discovery of the Potent, Highly Selective, Orally Available ATR Inhibitor BAY 1895344 with Favorable Pharmacokinetic Properties and Promising Efficacy in Monotherapy and in Combination Treatments in Preclinical Tumor Models. J Med Chem. 2020 Jul 9;63(13):7293-7325.

Elimusertib 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.66mL

0.53mL

0.27mL

13.32mL

2.66mL

1.33mL

26.64mL

5.33mL

2.66mL

Elimusertib 技术信息

CAS号1876467-74-1
分子式C20H21N7O
分子量 375.427
别名 BAY-1895344
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C
溶解度

DMSO: 4 mg/mL(10.65 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Elimusertib | 1876467-74-1 | BAY 1895344 | BAY1895344 | BAY-1895344 | ATR Inhibitor | Cell Cycle/DNA Damage | PI3K/Akt/mTOR | ATM/ATR | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Elimusertib 纯度/质量文件 | Elimusertib 亚型比较 | Elimusertib 生物活性 | Elimusertib 动物研究 | Elimusertib 参考文献 | Elimusertib 实验方案 | Elimusertib 技术信息

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