AT13148

Catalog No.S7563

For research use only.

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

CAS No. 1056901-62-2

Selleck's AT13148 has been cited by 10 Publications

1 Customer Review

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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)
Click to View More Targets
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells MW\GeY5kfGmxbjDhd5NigQ>? MnjSOVAhdWmwcx?= NWjJUWc{UW6qaXLpeIlwdiCxZjDOMZRmem2rbnHsJGhqey22YXfn[YQh\nWubD3s[Y5ofGhiaIXtZY4hemWlb33ibY5idnRicEewV|ZMKGW6cILld5Nm\CCrbjDTdI9ld3C2ZYLhJIZzfWercHXy[IEhcW6|ZXP0JINmdGy|IIXzbY5oKEGNUmLSUHNUVFKDIIP1ZpN1emG2ZTDhcoQh[W6mIGvnZY1u[S1|M2CtRXRRZSCrbnP1ZoF1\WRiZn;yJFUxKG2rboOgZpkhe2OrboTpcIxifGmxbjDjc5VvfGmwZzDt[ZRpd2RuIFnDOVA:OC5yMUNOwG0v MmPKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMN|U1PDl4MD:nQmNpTU2ETEyvZV4>
U87MG M4H5fGZ2dmO2aX;uJIF{e2G7 M2XwWFEhcHJ? M4LjSmlvcGmkaYTpc44hd2ZiUFvCJIlvKGi3bXHuJHU5P02JIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDpckBIe2t|YnX0ZUBU\XJ7IIDoc5NxcG:{eXzheIlwdiCrbnP1ZoF1\WRiZn;yJFEhcHJiYomgeIlu\S2{ZYPvcJZm\CCobIXvdoV{[2WwY3WgZoF{\WRiYYPzZZktKEmFNUC9NU4y|ryPLh?= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyzOVQ1QTZyLze+R4hGVUKOPD;hQi=>
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 (from reference)

Kinase Assay:

[1]

  • 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]

  • 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]

  • Animal Models: Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC(=CC=C1C2=CNN=C2)C(CN)(C3=CC=C(C=C3)Cl)O

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01585701 Completed Biological: AT13148 Advanced Solid Tumours Cancer Research UK May 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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