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: 1056901-62-2

Selleck's AT13148 has been cited by 12 Publications

1 Customer Review

Purity & Quality Control

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

Other Akt Products

Related compound libraries

Choose Selective Akt Inhibitors

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 lnformation & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy AT13148 | AT13148 supplier | purchase AT13148 | AT13148 cost | AT13148 manufacturer | order AT13148 | AT13148 distributor