ATR Degrader

PROTAC ATR degrader-3 is a potent CRBN-based ATR PROTAC degrader with a DC₅₀ of 127 nM. PROTAC ATR degrader-3 also degrades CHK1 with an DC₅₀ of 135 nM. PROTAC ATR degrader-3 inhibits cancer cells proliferation, migration and invasion, triggers apoptosis and induces S phase arrest and DNA damage. PROTAC ATR degrader-3 achieves tumor growth inhibition in LoVo xenograft mouse model without apparent toxicity. PROTAC ATR degrader-3 can be used for the research of colorectal cancer.

PROTAC ATR degrader-1 is a ATR PROTAC degrader. PROTAC ATR degrader-1 promotes ubiquitination and degradation of ATR. PROTAC ATR degrader-1 facilitates the progression of cells through the G2/M phase, thereby impairing DNA repair and inducing Apoptosis. PROTAC ATR degrader-1 exerts anticancer effects against colorectal cancer either alone or in combination with Cisplatin (HY-17394). PROTAC ATR degrader-1 can be used in research related to colorectal cancer.

PROTAC ATR degrader-2 is a selective ATR PROTAC degrader. PROTAC ATR degrader-2 degrades ATR in acute myeloid leukemia (AML) cells MV-4-11 and MOLM-13, with DC₅₀ values of 22.9 nM and 34.5 nM, respectively. PROTAC ATR degrader-2 has an IC₅₀ of 29.6 nM against ATR, and its IC₅₀ values against ATM and PI3K are both greater than 2000 nM. PROTAC ATR degrader-2 induces apoptosis, DNA damage, and upregulates p53 expression. PROTAC ATR degrader-2 inhibits cancer cell proliferation through the kinase-independent function of ATR protein. PROTAC ATR degrader-2 is applicable to research related to acute myeloid leukemia.