5.06387

gp130 Inhibitor, SC144

• Synonim(y): gp130 Inhibitor, SC144, SC144
• Wzór empiryczny (zapis Hilla): C₁₆H₁₁FN₆O · xHCl
• Masa cząsteczkowa: 322.30 (free base basis)
• Kod UNSPSC: 12352200
• Identyfikator substancji w PubChem: 66921431
• NACRES: NA.77

Właściwości

• Próba: ≥98% (HPLC)
• Poziom jakości: 100
• Postać: solid
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: light yellow
• rozpuszczalność: DMSO: 100 mg/mL
• temp. przechowywania: 2-8°C
• ciąg SMILES: C1=CN2C3=C(C=C(C=C3)F)N=C(C2=C1)NNC(=O)C4=NC=CN=C4.Cl

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Primary Target
gp130

Ostrzeżenie

Toxicity: Standard Handling (A)

Inne uwagi

Xu, S., et al. 2013. Mol. Cancer Ther.12, 937.

Informacje prawne

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3