5.06387
gp130 Inhibitor, SC144
Synonym(s):
gp130 Inhibitor, SC144, SC144
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About This Item
Empirical Formula (Hill Notation):
C16H11FN6O · xHCl
Molecular Weight:
322.30 (free base basis)
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
Assay
≥98% (HPLC)
Quality Level
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light yellow
solubility
DMSO: 100 mg/mL
storage temp.
2-8°C
SMILES string
C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4.Cl
General description
A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).
A cell-permeable, orally active, quinoxalinhydrazide derivative that acts an inhibitor of gp130. Binds to gp130 and induces its phosphorylation at Ser782 in ovarian cancer cells (OVCAR-8 and CaoV-3) in a time and dose-dependent manner. Shown to be cytotoxic in a number of ovarian cancer cell lines (IC50 = 720, 490, 950, 440, 530, 88-0, and 430 nM in OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY, and NCI/ADR-RES cells, respectively). Suppresses constitutive phosphorylation of and nuclear translocation of Stat3. Also blocks LIF and IL-6-induced Akt activation and phosphorylation of Stat3 (Y705) and Stat1 (Y701), without affecting their activation by IFN-γ. Reduces the level downstream effectors of gp130/Stat3 (survivin, MMP-7, Bcl-2, Bcl-xl, and cyclin D1) in ovarian cancer cells. Suppresses the growth of OVCAR-8 tumor xenografts in nude mice without affecting normal tissue (10 mg/kg, i.p. for 58 days).
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
Biochem/physiol Actions
Primary Target
gp130
gp130
Warning
Toxicity: Standard Handling (A)
Other Notes
Xu, S., et al. 2013. Mol. Cancer Ther.12, 937.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Certificates of Analysis (COA)
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