Flizasertib (GDC-8264) | RIPK1 inhibitor

Chemical Structure : Flizasertib

CAS No.: 2268739-68-8

Flizasertib (GDC-8264, GDC8264)

Catalog No.: 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.

Packing	Price	Stock
2 mg	$398	In stock
5 mg	$598	In stock
10 mg	$898	In stock
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Biological Activity

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.

Physicochemical Properties

M.Wt	271.30
Formula	C15H14FN3O
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
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

References

1. Patent WO2022212809 A1

Flizasertib (GDC-8264, GDC8264)

Biological Activity

Physicochemical Properties

References

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