| Identification | Back Directory | [Name]
Cyclopentanecarboxamide, 3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethyl-, (1R,3R)- | [CAS]
2396465-33-9 | [Synonyms]
GCN2-IN-7
Cyclopentanecarboxamide, 3-[[3-bromo-1-[4-(5-methyl-1,3,4-thiadiazol-2-yl)phenyl]-1H-pyrazolo[3,4-d]pyrimidin-6-yl]amino]-N,1-dimethyl-, (1R,3R)- | [Molecular Formula]
C22H23BrN8OS | [MOL File]
2396465-33-9.mol | [Molecular Weight]
527.44 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]. | 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. |
| [storage]
Store at -20°C | [References]
[1] Jackson JJ, et al. Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy. J Med Chem. 2022 Sep 20. DOI:10.1021/acs.jmedchem.2c00736 |
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