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Cat. No.: HY-184499

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GRWD5769

GRWD5769 is an oral 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 ameliorates T cell exhaustion. GRWD5769 is applicable to 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, cervical cancer, and lung cancer.

For research use only. We do not sell to patients.

CAS No.: 2420554-24-9
Formula: C₂₂H₂₂ClN₃O₄S
Molecular Weight:459.95

Storage:

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

GRWD5769 Chemical Structure

CAS No.: 2420554-24-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

MHC I

ERAP1

All MHC Isoforms :

MHC I
MHC II

All Aminopeptidase Isoforms :

CD13
LTA4H

Chemical Information

CAS No. 2420554-24-9
Molecular Weight 459.95
Formula C₂₂H₂₂ClN₃O₄S
SMILES

ClC(C=C1N2CCCCC2)=C(C#N)C=C1NS(C3=CC(C(O)=O)=CC=C3C4CC4)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

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.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
Chemical Information
Purity & Documentation
References

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GRWD5769

All MHC Isoforms

All Aminopeptidase Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

GRWD5769 Related Classifications

HY-184499 Related Classifications