3063346-83-5
Chemical Structure
LRK-4189
- CAS No.: 3063346-83-5
- Formula:C43H49F2N9O4
- Molecular Weight:793.90
IUPAC Name: (1S,4R)-4-(4-(4-(((S)-2,6-dioxopiperidin-3-yl)amino)-2-fluorophenyl)piperazin-1-yl)-N-((1r,4R)-4-((5-fluoro-4-(3-(2-oxopyridin-1(2H)-yl)phenyl)pyrimidin-2-yl)amino)cyclohexyl)cyclohexane-1-carboxamide
InChIKey: JESQZBCEODMQQE-CKZBKQOKSA-N
SMILES: 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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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- [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.
Keywords
