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United States

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Cat. No.: 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.

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CAS No.: 2420554-24-9
화학식: C₂₂H₂₂ClN₃O₄S
분자량:459.95

보관:

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

GRWD5769 Chemical Structure

CAS No.: 2420554-24-9

사이즈

가격

재고

수량

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[1]

MHC I

ERAP1

All MHC Isoforms :

MHC I
MHC II

All Aminopeptidase Isoforms :

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

CAS No. 2420554-24-9
분자량 459.95
화학식 C₂₂H₂₂ClN₃O₄S
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

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

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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CAS No.:
Species:
Purity:
수량:

GRWD5769

All MHC Isoforms

All Aminopeptidase Isoforms

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

GRWD5769 Related Classifications

HY-184499 Related Classifications