AZD5582

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Clon N/A
Menge 5mg
ArtNr HY-12600-5mg
Eclass 6.1 30220300
Eclass 9.0 32160605
Lieferbar
Synonyms
AZD-5582
CAS No.
1258392-53-8
Purity
>98%
MW
1015289
Formula
C58H78N8O8
Solubility
DMSO: >= 66.25 mg/mL
Biological Description
AZD5582 is a novel class of dimeric Smac mimetics as potent IAP antagonist; binds potently to the BIR3 domains of cIAP1, cIAP2, and XIAP (IC50 = 15, 21, and 15 nM, respectively).
IC50 value: 15/21/15 nM (cIAP1/cIAP2/XIAP) [1]
Target: IAPs inhibitor
AZD5582 causes cIAP1 degradation and induces apoptosis in the MDA-MB-231 breast cancer cell line at subnanomolar concentrations in vitro. When administered intravenously to MDA-MB-231 xenograft-bearing mice, AZD5582 results in cIAP1 degradation and caspase-3 cleavage within tumor cells and causes substantial tumor regressions following two weekly doses of 3.0 mg/kg. Antiproliferative effects are observed with AZD5582 in only a small subset of the over 200 cancer cell lines examined, consistent with other published IAP inhibitors [1]. AZD5582 significantly enhanced apoptosis induced by the death receptor (DR) agonist tumour necrosis factor-related apoptosis-inducing ligand (TRAIL). Importantly, killing by TRAIL plus AZD5582 was independent of adverse prognostic features including TP53 deletion which is strongly associated with chemoresistance in CLL [2].
Free  Sample
Available in quantities of 0, 5mg-1mg. Three different samples per customer per year!

Sicherheitsdatenblatt

HY-12600-5mg.pdf

Menge: 5mg
Lieferbar: In stock
Listenpreis: 165,71 €
Rabatt: -10,0%
Preis: 149,14 €
Sie sparen: 16,57 €
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