Elimusertib 是一种可口服的选择性ATR抑制剂,IC50值为 7 nM。它具有抗肿瘤活性,可研究实体瘤和淋巴瘤。
产品描述
BAY 1895344 is a potent, highly selective and orally available ATR inhibitor with an IC50 of 7 nM.BAY 1895344 shows potent anti-tumor efficacy in monotherapy and strong combination potential with the targeted alpha therapy Radium-223 dichloride.
体内活性
The novel selective ATR kinase inhibitor BAY 1895344 on tumor cell growth and viability.?Potent antiproliferative activity was demonstrated in a broad spectrum of human tumor cell lines.?BAY 1895344 exhibited strong monotherapy efficacy in cancer xenograft models that carry DNA damage repair deficiencies.?The combination of BAY 1895344 with DNA damage-inducing chemotherapy or external beam radiotherapy (EBRT) showed synergistic antitumor activity.?Combination treatment with BAY 1895344 and DDR inhibitors achieved strong synergistic antiproliferative activity in vitro, and combined inhibition of ATR and PARP signaling using olaparib demonstrated synergistic antitumor activity in vivo Furthermore, the combination of BAY 1895344 with the novel, nonsteroidal androgen receptor antagonist darolutamide resulted in significantly improved antitumor efficacy compared with respective single-agent treatments in hormone-dependent prostate cancer,?and addition of EBRT resulted in even further enhanced antitumor efficacy[1].
Cas No.
1876467-74-1
分子式
C20H21N7O
分子量
375.436
别名
BAY-1895344
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years