Anaplastic lymphoma kinase (ALK) Degrader

PROTAC ALK degrader-3 is an orally active ALK PROTAC degrader with a DC₅₀ of 119.33 nM in Karpas 299 cells. PROTAC ALK degrader-3 induces the degradation of ALK fusion proteins via the ubiquitin-proteasome system. PROTAC ALK degrader-3 induces NPM-ALK degradation and inhibits the expression of p-ALK and p-STAT3. PROTAC ALK degrader-3 inhibits cancer cell proliferation and suppresses the growth of xenografts in vivo. PROTAC ALK degrader-3 can be used for the research of ALK-positive cancers (e.g., anaplastic large cell lymphoma).

dALK-3 is an anaplastic lymphoma kinase (ALK) degrader. dALK-3 can effectively induce EML4-ALK degradation with a DC₅₀ of 0.182 μM. dALK-3 has good anti-proliferation activity against H3122 cells and can be used in the study of cancer.

PROTAC ALK5 Degrader-1 is a selective ALK5 PROTAC degrader. PROTAC ALK5 Degrader-1 induces ALK5 degradation via ALK5 ATP-binding pocket engagement, CRBN recruitment, and the ubiquitin-proteasome system.PROTAC ALK5 Degrader-1 inhibits ALK5 downstream signaling. PROTAC ALK5 Degrader-1 can be used for the research of pulmonary fibrosis.

PROTAC EML4-ALK Degrader-1 (Pro-BA) is an orally active EML4-ALK PROTAC degrader that recruits GID4, with a K_d value of 144 nM against human EML4-ALK and a DC₅₀ of 74 nM in H3122 cells. PROTAC EML4-ALK Degrader-1 promotes EML4-ALK ubiquitination and proteasomal degradation, reduces cancer cell viability, inhibits cancer cell and tumor growth, induces apoptosis, and alters cell cycle distribution. PROTAC EML4-ALK Degrader-1 can be used in studies related to EML4-ALK-positive cancers and non-small cell lung cancer.