Home PI3K/Akt/mTOR Akt inhibitor - S6 Kinase inhibitor - ROCK inhibitor - PKA inhibitor AT13148 For research use only.

AT13148

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.

AT13148 Chemical Structure

AT13148 Chemical Structure

CAS No. 1056901-62-2

Purity & Quality Control

Batch: S756301 DMSO]62 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.87%
99.87

AT13148 Related Products

Signaling Pathway

Akt Signaling Pathways

Akt Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells Function assay 50 mins Inhibition of N-terminal His-tagged full-length human recombinant p70S6K expressed in Spodoptera frugiperda insect cells using AKRRRLSSLRA substrate and and [gamma-33P-ATP] incubated for 50 mins by scintillation counting method, IC50=0.012μM. ChEMBL
U87MG Function assay 1 hr Inhibition of PKB in human U87MG cells assessed as reduction in Gsk3beta Ser9 phosphorylation incubated for 1 hr by time-resolved fluorescence based assay, IC50=1.1μM. ChEMBL
Click to View More Cell Line Experimental Data

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)		 Click to View More Targets
3 nM 4 nM 6 nM 8 nM 38 nM
In vitro
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]
Kinase Assay 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 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.
In Vivo
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]
Animal Research Animal Models Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
Dosages ~50 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01585701 Completed
Advanced Solid Tumours
Cancer Research UK
 May 2012 Phase 1

Chemical Information & Solubility

Molecular Weight 313.78 Formula

C17H16ClN3O
CAS No. 1056901-62-2 SDF Download AT13148 SDF
Smiles C1=CC(=CC=C1C2=CNN=C2)C(CN)(C3=CC=C(C=C3)Cl)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 62 mg/mL ( (197.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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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

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