895158-95-9

895158-95-9 structure

Name: SC144
Chemical Name: N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazi de
CAS Number: 895158-95-9
Molecular Formula: C₁₆H₁₁FN₆O
Molecular Weight: 322.297
Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
Create Date: 2016-06-28 22:34:50
Modify Date: 2024-02-05 14:02:37
SC144 is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.

Name	N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazi de
Synonyms	N'-(7-Fluoropyrrolo[1,2-a]quinoxalin-4-yl)-2-pyrazinecarbohydrazide 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide SC144

Description	SC144 is the first-in-class orally active small-molecule gp130 inhibitor; inhibits cell growth in a panel of human ovarian cancer cell lines with IC50 values in a submicromolar range.IC50 value: < 1 uM (Cell assay) [1]Target: gp130 inhibitorSC144 shows greater potency in human ovarian cancer cell lines than in normal epithelial cells. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. In addition, SC144 shows potent inhibition of gp130 ligand-triggered signaling. Oral administration of SC144 delays tumor growth in a mouse xenograft model of human ovarian cancer without significant toxicity to normal tissues.
Related Catalog	Signaling Pathways >> Immunology/Inflammation >> Interleukin Related Research Areas >> Cancer
References	[1]. Xu S, et al. Discovery of a novel orally active small-molecule gp130 inhibitor for the treatment of ovarian cancer. Mol Cancer Ther. 2013 Jun;12(6):937-49.