ATR Inhibitor

Ceralasertib (AZD6738) is an orally active and bioavailable inhibitor of ATR kinase with an IC₅₀ of 1 nM.

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

VE-821 is a potent ATP-competitive inhibitor of ATR with K_i/IC₅₀ of 13 nM/26 nM.

Elimusertib (BAY-1895344) is a potent, orally active and selective ATR inhibitor with an IC₅₀ of 7 nM. Elimusertib has anti-tumor activity. Elimusertib can be used for the research of solid tumors and lymphomas.

Camonsertib (RP-3500) is an orally active, selective ATR kinase inhibitor (ATRi) with an IC₅₀ of 1.00 nM in biochemical assays. Camonsertib shows 30-fold selectivity for ATR over mTOR (IC₅₀=120 nM) and >2,000-fold selectivity over ATM, DNA-PK, and PI3Kα kinases. Camonsertib has potent antitumor activity.

ATR-IN-31 is a selective ATR kinase inhibitor with an IC₅₀ of 7 nM. ATR-IN-31 does not significantly inhibit ATM kinase activity. ATR-IN-31 inhibits viability of prostate cancer cells.ATR-IN-31 can be used for the research of prostate cancer.

Gartisertib (VX-803) is an ATP-competitive, orally active, and selective ATR inhibitor, with a K_i of <150 pM. Gartisertib potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC₅₀ of 8 nM. Antitumor activity.

AZ20 is a potent and selective inhibitor of ATR with an IC₅₀ of 5 nM, and has 8-fold selectivity against mTOR (IC₅₀=38 nM).

Elimusertib (BAY 1895344) hydrochloride is a potent, orally active and selective ATR inhibitor with an IC₅₀ of 7 nM. Elimusertib hydrochloride has anti-tumor activity. Elimusertib hydrochloride can be used for the research of solid tumors and lymphomas.

CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer.

ETP-46464 is an effective mTOR and ATR inhibitor with IC₅₀s of 0.6 and 14 nM, respectively.

AD1058 is an orally active, selective, and BBB-permeable inhibitor of ATR (IC₅₀: 1.6 nM). AD1058 exhibits anticancer activity by inhibiting tumor cell proliferation, inducing cell cycle arrest, and promoting apoptosis. AD1058 is suitable for research on advanced malignancies and brain metastases.

NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with K_is of 2.5 μM and 1.3 μM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner.

Abd110 (compound 42i) is a Lenalidomide-based PROTAC ATR kinase degrader. Abd110 selectively decreases ATR and phospho-ATR without affecting related kinases ATM and DNA-PKcs.

ATR-IN-14 (compound 1) is a potent ATR kinase inhibitor. ATR-IN-14 inhibits ATR signaling pathways downstream CHKI protein phosphorylation, with inhibition of 98.03% at 25 nM. ATR-IN-14 shows good anticancer activity in LoVo cells, with an IC₅₀ of 64 nM.

ATR/PARP1-IN-1 is a potent ATR and PARP1 dual inhibitor with IC₅₀s of 17.3 nM and 0.38 nM, respectively. ATR/PARP1-IN-1 effectively reduces cell viability, induces apoptosis and DNA damage. ATR/PARP1-IN-1 significantly impairs triple-negative breast cancer (TNBC) colony formation, migration, and invasion. ATR/PARP1-IN-1 suppresses tumor growth effectively in MDA-MB-468 xenografted mice, with no significant body weight change.

ICT10336 is a hypoxia-responsive prodrug of ATR inhibitor, AZD6738 (HY-19323). ICT10336 is hypoxia-activated and specifically releases AZD6738 only in hypoxic conditions in vitro. This can inhibit ATR activation (T1989 and S428 phosphorylation) and subsequently abrogate HIF1a-mediated adaptation of hypoxic cancers cells, thus selectively inducing cell death in 2D and 3D cancer models. ICT10336 is a metabolic substrate of CYPOR activity.

ATR-IN-10 is a potent and highly selective inhibitor of ataxia telangiectasia mutated and Rad3-Related (ATR) kinase with an IC₅₀ value of 2.978 μM.

ATR-IN-19 (Compound 15 R-configure) is an 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.