AT13148

Catalog No.S7563

AT13148 Chemical Structure

Molecular Weight(MW): 313.78

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.

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1 Customer Review

  • 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.

    Biochem Biophys Res Commun, 2016, 478(1):330-6.. AT13148 purchased from Selleck.

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Biological Activity

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.
Targets
PKA [1]
(Cell-free assay)
ROCK2 [1]
(Cell-free assay)
ROCK1 [1]
(Cell-free assay)
p70S6K [1]
(Cell-free assay)
Akt1 [1]
(Cell-free assay)
3 nM 4 nM 6 nM 8 nM 38 nM
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. [1]

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. [1]

Protocol

Kinase Assay:

[1]

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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 Research:

[1]

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  • 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
  • Concentrations: ~10 μM
  • Incubation Time: 72 hours or 96 hours
  • Method:

    Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
  • Formulation: 10% DMSO, 1% Tween-20, and 89% saline
  • Dosages: ~50 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 62 mg/mL (197.59 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 313.78
Formula

C17H16ClN3O

CAS No. 1056901-62-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01585701 Recruiting Advanced Solid Tumours Cancer Research UK May 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID