| Identification | Back Directory | [Name]
5H-Pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide, 6,7-dihydro-5-phenyl-N-[(3R)-2,3,4,5-tetrahydro-7-methoxy-1-methyl-2-oxo-1H-pyrido[3,4-b]azepin-3-yl]-, (5R)-rel- | [CAS]
2438637-64-8 | [Synonyms]
5H-Pyrrolo[1,2-b][1,2,4]triazole-2-carboxamide, 6,7-dihydro-5-phenyl-N-[(3R)-2,3,4,5-tetrahydro-7-methoxy-1-methyl-2-oxo-1H-pyrido[3,4-b]azepin-3-yl]-, (5R)-rel- | [Molecular Formula]
C23 H24 N6 O3 | [MOL File]
2438637-64-8.mol | [Molecular Weight]
432.48 |
| Hazard Information | Back Directory | [Uses]
GNE684 is a potent inhibitor of potent receptor interacting protein 1 (RIP1), with mean Kiapp values of 21 nM, 189 nM and 691 nM for human mouse and rat RIP1, respectively[1]. | [in vivo]
GNE684 also had no impact on overall survival or tumor growth in the KPP or KPR (LSL-Kras G12D/+; p16/p19 fl/wt ; Trp53 R270H/wt ; Pdx1-cre) PDAC models[1].
GNE684 (50mg/kg; p.o. twice daily) inhibits colitis and ileitis caused by NEMO deficiency in intestinal epithelial cells (IECs)[1].
| Animal Model: | Nemofl/fl Villin.creERT2 mice (NEMO IEC-KO)[1] | | Dosage: | 50 mg/kg | | Administration: | Oral administration; twice daily; from days 2–6 treated with tamoxifen | | Result: | Almost completely protected the NEMO-deficient intestines from colitis and ileitis. |
| [References]
[1] Patel S, et al. RIP1 inhibition blocks inflammatory diseases but not tumor growth or metastases. Cell Death Differ. 2019 May 17. DOI:10.1038/s41418-019-0347-0 |
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