Name: AT13148
Brand: Selleck Chemicals
SKU: S7563
Availability: InStock
Rating: 5 (14 reviews)

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.87

Related Targets	PI3K mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
Other Akt Products	MK-2206 Dihydrochloride SC79 AZD5363 (Capivasertib) Ipatasertib (GDC-0068) Perifosine GSK690693 Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	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

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (197.59 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.100mg/ml (9.88mM)	Taking the 1 mL working solution as an example, add 50 μL of 62 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.440mg/ml (1.40mM)	Taking the 1 mL working solution as an example, add 50 μL of 8.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Chemical Information, Storage & Stability

Molecular Weight	313.78	Formula	C₁₇H₁₆ClN₃O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1056901-62-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=CC=C1C2=CNN=C2)C(CN)(C3=CC=C(C=C3)Cl)O

Mechanism of Action

Targets/IC₅₀/Ki	PKA (Cell-free assay) 3 nM ROCK2 (Cell-free assay) 4 nM ROCK1 (Cell-free assay) 6 nM p70S6K (Cell-free assay) 8 nM Akt1 (Cell-free assay) 38 nM Akt3 (Cell-free assay) 50 nM SGK3 (Cell-free assay) 63 nM RSK1 (Cell-free assay) 85 nM Akt2 (Cell-free assay) 402 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, this compound also inhibits AKT and p70S6K signaling.
Kinase Assay	In vitro kinase assays
Kinase Assay	AT13148 is assayed against 40 kinases and the percentage inhibition at 10 μM of this compound is determined. Individual IC50 values are measured for selected kinases using ATP concentrations equivalent to the Km for each enzyme.
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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/22781553/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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AT13148 Akt inhibitor

Chemical Structure

Molecular Weight: 313.78