1. Immunology/Inflammation
  2. CD73
  3. W-GTF01

W-GTF01 is a MGAT1 inhibitor. W-GTF01 blocks the MGAT1-catalyzed glycosylation of CD73, and inhibits CD73 dimerization, membrane translocation and adenosine production. W-GTF01 restores the function of IFNγ-producing CD8+ T cells, enhances tumor infiltration and activation of CD8+ T cells, and suppresses tumor growth. W-GTF01 can be used in research related to triple-negative breast cancer.

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

W-GTF01

W-GTF01 Chemical Structure

CAS No. : 951968-89-1

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Description

W-GTF01 is a MGAT1 inhibitor. W-GTF01 blocks the MGAT1-catalyzed glycosylation of CD73, and inhibits CD73 dimerization, membrane translocation and adenosine production. W-GTF01 restores the function of IFNγ-producing CD8+ T cells, enhances tumor infiltration and activation of CD8+ T cells, and suppresses tumor growth. W-GTF01 can be used in research related to triple-negative breast cancer[1][2].

In Vitro

W-GTF01 restores tumor immune response in immunosuppressive breast cancer cells and reduces CD73 membrane localization in MDA-MB468 and MDA-MB231 triple-negative breast cancer (TNBC) cells by blocking MGAT1-mediated CD73 glycosylation[1].
W-GTF01 potently and dose-dependently inhibits MGAT1 enzymatic activity via specific binding to the MGAT1 active site[2].
W-GTF01 revives CD8+ effector T cell function (including IFNγ production) and reduces MDA-MB468 TNBC cell survival in a CD73-dependent manner in 2D coculture with PBMCs[2].

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

In Vivo

W-GTF01 (5 mg/kg; i.p.; twice per week) sensitizes 4T1-hPD-L1 triple-negative breast cancer tumors to anti-PD-L1 therapy in BALB/C mice, enhancing tumor growth suppression, improving survival, increasing CD8+ T cell infiltration and activation, and reducing T cell exhaustion[2].

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

Animal Model: BALB/C (female; syngeneic triple-negative breast cancer model with 4T1-hPD-L1 cells injected subcutaneously into mammary fat pad)[2]
Dosage: 5 mg/kg
Administration: i.p.; twice per week
Result: Exhibited enhanced tumor growth suppression relative to single treatments.
Prominently improved survival outcomes compared with monotherapy and control groups.
Markedly elevated CD8+ T cell infiltration and activation and mitigated T cell exhaustion versus anti-PD-L1 antibody alone.
Molecular Weight

416.43

Formula

C24H20N2O5

CAS No.
SMILES

O=C(C1=CC(OCO2)=C2C=C1)NC3=CC(C4=NC5=C(C=C(C)C(C)=C5)O4)=C(O)C(C)=C3

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

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
W-GTF01
Cat. No.:
HY-185701
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