产品说明书

Elimusertib

Print
Chemical Structure| 1876467-74-1 同义名 : BAY-1895344
CAS号 : 1876467-74-1
货号 : A164508
分子式 : C20H21N7O
纯度 : 99%+
分子量 : 375.427
MDL号 : MFCD31561442
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.