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GCN2-IN-7 

Cat. No.: HY-151460
Handling Instructions

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo.

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

GCN2-IN-7 Chemical Structure

GCN2-IN-7 Chemical Structure

CAS No. : 2396465-33-9

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Description

GCN2-IN-7 (compound 39) is an orally active and selective general control nonderepressible 2 (GCN2) inhibitor (IC50=5 nM). GCN2-IN-7 shows anti-tumor activity in vivo[1].

IC50 & Target

IC50: 5 nM (GCN2)[1]

In Vitro

GCN2-IN-7 (600 nM; 3 d) alleviates myeloid-derived suppressive cells (MDSC)-related T cell suppression and restores T cell proliferation[1].

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

Cell Proliferation Assay[1]

Cell Line: CD8+ T cells from WT and GCN2KO cells
Concentration: 600 nM
Incubation Time: 3 days
Result: Relieved MDSC suppression of proliferation of the co-cultured CD8+ T cells with significant relief at 600 nM.
In Vivo

GCN2-IN-7 (oral gavage; 15 mg/kg; BID; 17 d) shows robust target engagement in vivo at a reasonable dose[1].
GCN2-IN-7 (oral gavage; 50 mg/kg; BID; 17 d) inhibits tumor growth in vivo of the LL2 syngeneic mouse tumor model[1].

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

Animal Model: Balb/c mice injected with RENCA cells[1]
Dosage: 15 mg/kg
Administration: Oral gavage; 15 mg/kg; BID; 17 days
Result: Showed robust target engagement of GCN2 in both tumor (average of 84%) and spleen (average of 80%) tissues.
Showed an average of 65% reduction of downstream marker Activation Transcription Factor 4 (ATF4) in compound-treated mice compared to the vehicle treatment group.
Animal Model: LL2 syngeneic mouse model[1]
Dosage: 50 mg/kg
Administration: Oral gavage; 50 mg/kg; BID; 17 days
Result: Showed tumor growth inhibition (56%) after 26 days of dosing compared to the vehicle group.
Molecular Weight

527.44

Formula

C22H23BrN8OS

CAS No.
SMILES

O=C([[email protected]@]1(C)C[[email protected]](NC2=NC=C3C(N(C4=CC=C(C5=NN=C(C)S5)C=C4)N=C3Br)=N2)CC1)NC

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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GCN2-IN-7
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HY-151460
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