LRK-4189 

LRK-4189 is an orally active PIP4K2C (a regulator of mTOR complex) degrader and type 1 immune activator. LRK-4189 induces the degradation of the lipid kinase PIP4K2C. LRK-4189 triggers the interferon signaling pathway in microsatellite-stable (MSS) colorectal cancer cells, activates immunogenic tumor killing, and induces endogenous cell death. LRK-4189 sensitizes microsatellite-stable colorectal cancer tumors to NK cell killing and dendritic cell phagocytosis. LRK-4189 can be used for the research of microsatellite-stable colorectal cancer^[1][2].

LRK-4189 (Compound 603) exhibits a 24 h DC₅₀ of <500 nM against PIP4K2C in MOLT-4 cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

793.90

C₄₃H₄₉F₂N₉O₄

3063346-83-5

O=C1CC[C@@H](C(N1)=O)NC2=CC=C(C(F)=C2)N3CCN(CC3)[C@H]4CC[C@@H](CC4)C(N[C@H]5CC[C@@H](CC5)NC6=NC(C7=CC=CC(N8C=CC=CC8=O)=C7)=C(C=N6)F)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. D’Hennezel E, Goodman K, O’Shea M, et al. 1281 LRK-4189, a first-in-class degrader of the lipid kinase PIP4K2C for the treatment of microsatellite stable (MSS) colorectal carcinoma[J]. 2025.

  [2]. Preparation of trisubstituted pyrimidine compounds as inhibitors and degraders of PIP4K protein. World Intellectual Property Organization, WO2024233846 A1.