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. |
![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)- Structure](/CAS/20210305/GIF/2396465-33-9.gif)
