DT-5461 is an IL-1 and TNF-alpha antagonist, with low endotoxicity and potent antitumor activity dissociated from toxic potential. DT-5461 competitively binds lipid A-binding sites on macrophage receptors, blocks LPS-initiated signaling, inhibits LPS-induced cytokine release, prevents LPS-induced serum cytokine production in mice, and protects against LPS-induced lethal endotoxemia. DT-5461 induces minimal cytokine production, inhibits tumor metastasis, prolongs tumor-bearing mouse survival, induces splenomegaly, avoids DIC induction, causes hepatocellular necrosis with repeated intravenous administration, induces endogenous TNF and interferon a/b, reduces tumor microcirculatory blood flow, augments tumor cell-induced TNF production, activates host immune systems, and exhibits activity against human tumor xenografts. DT-5461 has weaker activity against tumors linked to elevated host blood immunosuppressive factors, with rat lethality unaffected by injection speed but enhanced in partially hepatectomized or D-galactosamine-treated rats. DT-5461 can be used for the research of lethal endotoxemia, gram-negative bacterial septicemia, meth a fibrosarcoma, oat-cell lung carcinoma, medullary tubular mammary carcinoma, poorly differentiated colon adenocarcinoma, squamous-cell lung carcinoma, poorly differentiated gastric adenocarcinoma, and gelatinous gastric adenocarcinoma[1][2][3].
Molekulargewicht:
1449.82
CAS Nummer:
[123598-19-6]
Formel:
C73H133N4O22P
Target-Kategorie:
Interleukin Related,TNF Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound1
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
