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Referencia número: HY-184499

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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.

Para uso exclusivo en investigación. No vendemos a pacientes.

No. CAS: 2420554-24-9
Fòrmula: C₂₂H₂₂ClN₃O₄S
Peso molecular:459.95

Almacenamiento:

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

GRWD5769 Chemical Structure

No. CAS: 2420554-24-9

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Use of MCE Products

Fluorescent Dye

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

Actividad biológica
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- IC₅₀ & Target
- In Vitro
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Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target^[1]

MHC I

ERAP1

Ver todos los productos específicos de isoformas MHC :

MHC I
MHC II

Ver todos los productos específicos de isoformas Aminopeptidase :

CD13
LTA4H

In Vitro

Combination treatment with GRWD5769 and anti-PD-1 mAb (HY-P99144) increases intratumoral TCR repertoire diversity, promotes T cell infiltration, upregulates markers associated with immune responses as well as recently activated, non-exhausted T cells, and inhibits tumor growth across multiple syngeneic tumor models in different mouse strains.

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

Chemical Information

No. CAS 2420554-24-9
Peso molecular 459.95
Fòrmula C₂₂H₂₂ClN₃O₄S
SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento

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

Pureza y Documentación

Instrucciones de manejo (2659 KB)

Referencias

[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.

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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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- In Vitro
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GRWD5769

Ver todos los productos específicos de isoformas MHC

Ver todos los productos específicos de isoformas Aminopeptidase

Actividad biológica

Chemical Information

Pureza y Documentación

Referencias

Calculators

Help & FAQs

GRWD5769 Related Classifications

HY-184499 Related Classifications