2268739-68-8
Chemical Structure
Flizasertib
Synonym(s): GDC-8264
- CAS No.: 2268739-68-8
- Formula:C15H14FN3O
- Molecular Weight:271.29
IUPAC Name: sodium 4-(3-(4-hydroxy-3-methylphenyl)-1,1-dioxido-3H-benzo[c][1,2]oxathiol-3-yl)-2-methylphenolate
InChIKey: LMXPZWQVDDSYHH-RYUDHWBXSA-N
SMILES: F[C@@H]1C2=NC(C(C3CC3)=O)=NN2[C@H](C4=CC=CC=C4)C1
Biological Activity: Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with Kiapp values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Flizasertib | 99.9% | Flizasertib (GDC-8264) is an orally active, reversible and selective RIP1 inhibitor with Kiapp values of 0.00071 μM and 0.0013 μM for human and cynomolgus monkey RIP1 kinase, respectively. Flizasertib blocks RIP1 autophosphorylation but does not affect RIP1 protein stability. Flizasertib inhibits pro-inflammatory cytokines (CCL3, CCL4, and IL-1β) production. Flizasertib results in inhibition of colitis and ileitis. Flizasertib can be used in the research of cardiac surgery-associated acute kidney injury. | ||||||||||||||||||||
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- [1]. Patel S, et al. Discovery of Clinical Candidate GDC-8264, a Novel, Potent and Selective RIP1 Inhibitor for Amelioration of Tissue Damage and the Treatment of Inflammatory Diseases. J Med Chem. 2025;68(21):23050-23077. [Content Brief]
- [2]. Jones NS, et al. A phase I, randomized, ascending-dose study to assess safety, pharmacokinetics, and activity of GDC-8264, a RIP1 inhibitor, in healthy volunteers. Clin Transl Sci. 2023;16(10):1997-2009. [Content Brief]
Keywords
