Bioactivity | ATR-IN-23 (Compound 34) is a potent and selective ATR inhibitor with an IC50 of 1.5 nM. ATR-IN-23 has potent antiproliferative effects on LoVo cells and synthetic lethality on HT-29 cells, and can be used in the study of DNA damage response (DDR)-deficient cancers[1]. |
Invitro | ATR-IN-23 对 ATR 具有显著的抑制作用,IC50 值为 1.5 nM,对 LoVo 细胞显示出强的抗增殖活性,IC50 值为 0.073 μM[1]。ATR-IN-23 对 HT-29 细胞表现出中等的抗增殖效力,IC50 值为 0.161 μM[1]。 |
In Vivo | ATR-IN-23 在最大浓度为 2000 mg/kg 时表现出急性毒性,在 ICR 小鼠中具有中等安全性[1]。ATR-IN-23 (50 mg/kg;一天一次或一天两次;p.o.;21 天) 在 BALB/c 裸鼠中表现出中等抗肿瘤功效[1]。 Animal Model: |
Name | ATR-IN-23 |
Formula | C20H22N6O3S2 |
Molar Mass | 458.56 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Duan Y, et al. Discovery of Thieno[3,2-d]pyrimidine derivatives as potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) kinase. Eur J Med Chem. 2023 Jul 5;255:115370. |