Cas No.: | 895158-95-9 |
Synonyms: | SC144,SC-144,SC 144 |
SMILES: | O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3 |
Formula: | C16H11FN6O |
M.Wt: | 322.3 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
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.SC144 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. |
Target: | gp130 inhibitor IC50 value: < 1 uM (Cell assay) [1] |
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. |