917497-70-2
917497-70-2 structure
- Name: SC 144 hydrochloride
- Chemical Name: 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide, hydrochloride
- CAS Number: 917497-70-2
- Molecular Formula: C16H12ClFN6O
- Molecular Weight: 358.75700
- Catalog: Signaling Pathways Immunology/Inflammation Interleukin Related
- Create Date: 2016-09-26 10:47:10
- Modify Date: 2024-01-03 12:32:21
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SC144 hydrochloride 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 | 2-Pyrazinecarboxylic acid, 2-(7-fluoropyrrolo[1,2-a]quinoxalin-4-yl)hydrazide, hydrochloride |
|---|---|
| Synonyms |
SC 144 hydrochloride
SC144 (hydrochloride) |
| Description | SC144 hydrochloride 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. |
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| Related Catalog | |
| References |
| Melting Point | 282 °C (decomp) (methanol) |
|---|---|
| Molecular Formula | C16H12ClFN6O |
| Molecular Weight | 358.75700 |
| Exact Mass | 358.07500 |
| PSA | 84.21000 |
| LogP | 3.43940 |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| RIDADR | NONH for all modes of transport |