Flizasertib (GDC-8264) | RIPK1 inhibitor | Probechem Biochemicals

Chemical Structure : Flizasertib

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Flizasertib (GDC-8264, GDC8264)

货号: PC-20036Not For Human Use, Lab Use Only.

Flizasertib (GDC-8264) is a potent, selective receptor-interacting protein 1 (RIP1, RIPK1) inhibitor with Kiapp of 0.71 nM.

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生物&药学活性

Flizasertib (GDC-8264) is a potent, selective receptor-interacting protein 1 (RIP1, RIPK1) inhibitor with Kiapp of 0.71 nM.

GDC-8264 more potently inhibits the kinase activity of primate RIP1 (human Kiapp = 0.00071 μM and cyno Kiapp = 0.0013 μM) than rodent orthologs (mouse Kiapp = 4.5 μM and rat Kiapp > 10 μM).

GDC-8264 blocks RIP1 autophosphorylation but did not affect RIP1 protein stability or TNF-stimulated NF-κB and MAPK activation and the induction of gene expression.

GDC-8264 potently inhibits cell death in immortalized human HT29 cells with IC50 of 7.8 nM.

GDC-8264 inhibits TBZ-stimulated CCL3, CCL4, and IL-1β production in human whole blood with IC50 of < 2 nM.

GDC-8264 inhibits colon and ileum crypt damage and inflammation in NEMO IEC cKO mice, inhibits TNF plus zVAD (TZ)-driven SIRS (systemic inflammatory response syndrome) mouse model.

物理化学性质&存储条件

分子量	271.30
分子式	C15H14FN3O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Cyclopropyl[(5S,7S)-7-fluoro-6,7-dihydro-5-phenyl-5H-pyrrolo[1,2-b][1,2,4]triazol-2-yl]methanone

参考文献

1. Patent WO2022212809 A1

Flizasertib (GDC-8264, GDC8264)

生物&药学活性

物理化学性质&存储条件

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Flizasertib (GDC-8264, GDC8264)

生物&药学活性

物理化学性质&存储条件

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