ATR Inhibitor

ATR-IN-15 (compound 1) is an orally active and potent ATR kinase inhibitor, with an IC₅₀ of 8 nM. ATR-IN-15 also inhibits human colon tumor cells LoVo, DNA-PK and PI3K, with IC₅₀ values of 47, 663 and 5131 nM, respectively.

ATR-IN-21 (compound 60) is a potent ATR inhibitor with an IC₅₀ value of <1000 nM.

ATR-IN-17 (compound 88) is a potent ATR kinase inhibitor. ATR-IN-17 shows good anticancer activity in LoVo cells, with an IC₅₀ of 1 nM.

ATR-IN-20 is a potent ATR (ATM/ATR) inhibitor with an IC₅₀ of 3 nM. ATR-IN-20 possess an inhibitory effect on mTOR (IC₅₀ of 18 nM) while displaying good selectivity against PI3Kα (100 nM), ATM (100 nM), and DNA-PK (662 nM). ATR-IN-20 exhibits excellent pharmacokinetic profile (F = 30%), and has anticancer effects.

Antitumor agent-28 selectively inhibits ataxia telangiectasia mutated (ATM) kinase. Antitumor agent-28 prevents ATM mediated disease and has potent anti-cancer activity.

ATR-IN-29 is a potent and orally active ATR kinase inhibitor with an IC₅₀ value of 1 nM. ATR-IN-29 shows antiproliferative activity.

ATR-IN-13 (compound A9) is a potent ATR kinase inhibitor, with an IC₅₀ of 2 nM. ATR-IN-13 can be used for ATR kinase mediated diseases research, such as proliferative diseases and cancer.

Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G₂/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer.

ATR-IN-18 (compound 2) is an orally active and potent ATR kinase inhibitor, with an IC₅₀ of 0.69 nM. ATR-IN-18 shows antiproliferative activity in LoVo cells, with an IC₅₀ of 37.34 nM. ATR-IN-18 has anti-tumor activity.

ATR-IN-33 is an ATR kinase inhibitor (IC₅₀ = 9.67 nM). ATR-IN-33 induces apoptosis, exacerbates DNA damage, and causes G1 phase cell cycle arrest by blocking CHK1 phosphorylation and DNA damage response signaling. ATR-IN-33 exhibits selective cytotoxicity against AML cell lines and can be used for research on acute myeloid leukemia.

ATR-IN-16 (compound 46) is a potent ATR kinase inhibitor. ATR-IN-16 shows good anticancer activity in LoVo cells, with an IC₅₀ of 410 nM.