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Cat. No.: HY-172934

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FGT-4

FGT-4 is a FR-β-targeted chimeric molecule. FGT-4 acts as a TLR7 agonist. FGT-4 binds to FR-β to enable delivery to tumor-associated macrophages and myeloid-derived suppressor cells. FGT-4 promotes the secretion of iNOS (associated with M1 macrophages) and the pro-inflammatory cytokine IL-6, and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 can be used for the research of breast cancer.
(Pink: TLR7 ligand (HY-103698); Blue: FR-β ligand (HY-172935); Black: linker (HY-172936)).

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

Formula: C₅₀H₅₇N₁₁O₉S₂
Molecular Weight:1020.19

Storage:

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

Data Sheet (270 KB)

FGT-4 Chemical Structure

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Use of MCE Products

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

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

Biological Activity

Description

FGT-4 is a FR-β-targeted chimeric molecule. FGT-4 acts as a TLR7 agonist. FGT-4 binds to FR-β to enable delivery to tumor-associated macrophages and myeloid-derived suppressor cells. FGT-4 promotes the secretion of iNOS (associated with M1 macrophages) and the pro-inflammatory cytokine IL-6, and enhances the proliferation of cytotoxic CD8+ T cells. FGT-4 can be used for the research of breast cancer^[1]. (Pink: TLR7 ligand (HY-103698); Blue: FR-β ligand (HY-172935); Black: linker (HY-172936)).

IC₅₀ & Target^[1]

FR-β

TLR7

IL-6

iNOS

All Toll-like Receptor (TLR) Isoforms :

All NO Synthase Isoforms :

All Interleukin Related Isoforms :

In Vitro

FGT-4 (24 h) exhibits minimal cytotoxicity to 4T1 breast cancer cells and HUVEC cells across a broad concentration range^[1].

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

In Vivo

FGT-4 (1 mg/kg; i.v.; daily; 14 days) inhibits 4T1 tumor growth, reprograms tumor-associated macrophages to a pro-inflammatory phenotype, reshapes the tumor immune microenvironment, extends mouse survival to 35 days, and exhibits no apparent systemic toxicity^[1].
FGT-4 (20 μg; s.c.; single dose) does not induce elevated pro-inflammatory cytokine levels in healthy mice, demonstrating improved safety compared to free IMDQ^[1].

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

Animal Model:

BALB/c (female, 6 weeks old, orthotopic 4T1 tumor model, fed 2-week folate-deficient diet)^[1]
Dosage:

1 mg/kg
Administration:

i.v.; daily; 14 days
Result:

Reduced tumor growth compared to control group, with final tumor weights lower than control.
Increased the M1/M2 macrophage ratio in tumor tissues.
Decreased the proportion of Ly6C⁺ and Ly6G⁺ myeloid-derived suppressor cells within CD45⁺ cells.
Upregulated the percentage of CD8⁺ T cells in tumors.
Extended mouse survival to 35 days.
Caused no significant changes in mouse body weight during treatment.
Detected no pathological alterations in heart, liver, spleen, or kidney tissues.

Animal Model:

BALB/c (female, 6 weeks old)^[1]
Dosage:

20 μg
Administration:

s.c.; single dose
Result:

Did not trigger increased plasma levels of TNF-α or IL-6.

Chemical Information

Molecular Weight 1020.19
Formula C₅₀H₅₇N₁₁O₉S₂
SMILES

NC(NC1=O)=NC2=C1C=C(CCCCC3=CC=C(C=C3)C(N[C@H](C(O)=O)CCC(N[C@H](C(O)=O)CSSCCOC(NCC4=CC=C(CN5C6=C7C=CC=CC7=NC(N)=C6N=C5CCCC)C=C4)=O)=O)=O)N2
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Guo L, et al. Design and Synthesis of FR-β Targeting Chimeric Molecules for Reprogramming Tumor-Associated Macrophages Using 6-Substituted Pyrrolo[2,3-d]pyrimidines as Targeting Ligands. J Med Chem. 2025 Apr 24;68(8):8295-8309. [Content Brief]

Calculators

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

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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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

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

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FGT-4

All Toll-like Receptor (TLR) Isoforms

All NO Synthase Isoforms

All Interleukin Related Isoforms