|Solubility (25°C) *||In vitro||DMSO||62 mg/mL (197.59 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||AT13148 is an oral, ATP-competitive, multi-AGC kinase inhibitor with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM for Akt1/2/3, p70S6K, PKA, and ROCKI/II, respectively. Phase 1.|
|In vitro||AT13148, as a multi-AGC kinase inhibitor, potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines with deregulation of PI3K-AKT-mTOR or RAS-RAF pathways. In PTEN-deficient MES-SA cells, AT13148 also inhibits AKT and p70S6K signaling. |
|In vivo||AT13148 (50 mg/kg p.o.) markedly inhibits the activity of both AKT and p70S6K AGC kinases, and subsequently exhibits marked antitumor effects in human tumor xenografts. |
|In vitro kinase assays||AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of AT13148 is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.|
|Cell lines||MES-SA, MES-SA/Dx5, BT474, HCT-116, A549, PC3, SK-BR-3, MCF7, U87MG, MDA-MB-468, DU-145, and SK-OV-3 cell lines|
|Incubation Time||72 hours or 96 hours|
Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay.
|Animal Models||Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts|
|Formulation||10% DMSO, 1% Tween-20, and 89% saline|
Data from [Data independently produced by , , Biochem Biophys Res Commun, 2016, 478(1):330-6.]
AT13148 exerts cytotoxic and anti-proliferative activity against human gastric cancer cells. Human gastric cancer cells (HGC-27, AGS, SNU-601, N87 and MKN-28 lines) or GEC-1 gastric epithelial cells were treated with applied concentration of AT13148 for indicated time, cell survival (A and E), cell proliferation (B and F), cell cycle distribution (C, for HGC-27 cells) and cell death (D, for HGC-27 cells) were tested by the described assays, separately. Data were presented as mean ± SD. “Ctrl” stands for untreated control cells (For all figures). “hr/hrs” stands for hour/hours (For all figures). Experiments in this figure were repeated for five times. *p < 0.05 vs. “Ctrl” group.
Upregulation of programmed cell death ligand 1 promotes resistance response in non-small-cell lung cancer patients treated with neo-adjuvant chemotherapy. [Zhang P, et al. Cancer Sci, 2016, 107(11):1563-1571]PubMed: 27581532
AT13148, a first-in-class multi-AGC kinase inhibitor, potently inhibits gastric cancer cells both in vitro and in vivo [Xi Y, et al. Biochem Biophys Res Commun, 2016, 478(1):330-6]PubMed: 26828267
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