10mM in DMSO für empfindliche chromatographische und analytische Workflows, die minimale Basislinieninterferenzen erfordern.
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In 0 peer-reviewten Publikationen zu Chromatographie, organischer Synthese und Kreuzkupplungsreaktionen zitiert.
Information
AT7867 is a potent ATP-competitive inhibitor ofAkt1/2/3andp70S6K/PKAwithIC50of 32 nM/17 nM/47 nM and 85 nM/20 nM in cell-free assays, respectively; little activity outside the AGC kinase family.
In vitro
AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50 of 20 nM and 85 nM, respectively. AT7867 shows ATP-competitive activity to Akt2 with Ki of 18 nM. AT7867 exhibits antiproliferation in cell lines with PTEN or PIK3CA mutations and shows great potent to MES-SA, MDA-MB-468, MCF-7, HCT116 and HT29 with IC50 of 0.94 μM, 2.26 μM, 1.86 μM, 1.76 μM and 3.04 μM, respectively. AT7867 also suppresses the cell growth of U87MG, PC-3 and DU145 cells with IC50 of 8.22 μM, 10.37 μM and 11.86 μM, respectively. AT7867 suppresses Akt activity by inhibiting phosphorylation of GSK-3β in human tumor cells with IC50 of 2-4 μM. AT7867 also induces the phosphorylation of the following Akt direct substrates including proapoptotic transcription factors FKHR (FoxO1a), FKHRL1 (FoxO3a) and the downstream target S6RP in U87MG cells.
In vivo
AT7867 shows bioavailability of 44% in mice by p.o. route. AT7867 could increase the cleaved PARP in MES-SA xenografts at 20 mg/kg i.p. or 90 mg/kg p.o.. AT7867 significantly inhibits the tumor growth in MES-SA xenografts or U87MG xenografts with T/C of 0.37 and 0.51, respectively.
Cell Data
cell lines：
Concentrations：0-100 μM , dissolved to a 10 mM stock in DMSO
Incubation Time：
Powder Purity:≥95%
Umfassendes Dokument zu Gefahren, Handhabung, Lagerung und Einhaltung regulatorischer Vorschriften.
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Spezifikationsblatt ansehen →| Löslichkeit | Solubility (25°C) In vitro DMSO: 100 mg/mL (354.24 mM); |
|---|---|
| Siedepunkt (°C) | 530.2 °C/760 mmHg |
