2420554-24-9
Chemical Structure
GRWD5769
- CAS No.: 2420554-24-9
- Formula:C22H22ClN3O4S
- Molecular Weight:459.95
InChIKey: RATCWDMJKZPCKO-UHFFFAOYSA-N
SMILES: ClC(C=C1N2CCCCC2)=C(C#N)C=C1NS(C3=CC(C(O)=O)=CC=C3C4CC4)(=O)=O
Biological Activity: GRWD5769 is an orally potent ERAP1 inhibitor. GRWD5769 regulates the peptide repertoire presented by MHC-I, alters TCR diversity/clonality, reprograms antigen-experienced T cells, induces novel T cell responses, drives tumor cell killing, and alleviates T cell exhaustion. GRWD5769 can be used in the research of advanced solid malignancies, microsatellite-stable colorectal cancer, non-small cell lung cancer, bladder cancer, hepatocellular carcinoma, head and neck squamous cell carcinoma, and cervical cancer[1][2].
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GRWD5769 | GRWD5769 is an orally potent ERAP1 inhibitor. GRWD5769 regulates the peptide repertoire presented by MHC-I, alters TCR diversity/clonality, reprograms antigen-experienced T cells, induces novel T cell responses, drives tumor cell killing, and alleviates T cell exhaustion. GRWD5769 can be used in the research of advanced solid malignancies, microsatellite-stable colorectal cancer, non-small cell lung cancer, bladder cancer, hepatocellular carcinoma, head and neck squamous cell carcinoma, and cervical cancer. | |||||||||||||||||||||
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References
- [1]. Lillie T, et al. EMITT-1: Proof-of-mechanism immunopeptidome effects at target PK exposure, in a phase 1 study of GRWD5769 in patients with solid malignancies. ASCO Poster Session 2589. 2024.
- [2]. Thistlethwaite F, et al. EMITT-1: Clinical and pharmacodynamic activity with the oral ERAP1 inhibitor GRWD5769 and cemiplimab in 6 completed phase 1b expansion cohorts in solid tumors with anti-PD-1 resistance or MSS-CRC. ASCO Oral Abstract Session 2500. 2026.
