1. PI3K/Akt/mTOR
    Stem Cell/Wnt
    Protein Tyrosine Kinase/RTK
    TGF-beta/Smad
    Cell Cycle/DNA Damage
    MAPK/ERK Pathway
  2. Akt
    PKA
    ROCK
    Ribosomal S6 Kinase (RSK)
  3. AT13148

AT13148 

Cat. No.: HY-16071 Purity: 99.54%
Handling Instructions

AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s 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.

For research use only. We do not sell to patients.

AT13148 Chemical Structure

AT13148 Chemical Structure

CAS No. : 1056901-62-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 160 In-stock
Estimated Time of Arrival: December 31
5 mg USD 145 In-stock
Estimated Time of Arrival: December 31
10 mg USD 245 In-stock
Estimated Time of Arrival: December 31
50 mg USD 645 In-stock
Estimated Time of Arrival: December 31
100 mg USD 945 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

AT13148 is an orally active and ATP-competitive, multi-AGC kinase inhibitor with IC50s 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.

IC50 & Target[1]

Akt1

38 nM (IC50)

Akt3

50 nM (IC50)

Akt2

402 nM (IC50)

PKA

3 nM (IC50)

ROCKII

4 nM (IC50)

ROCKI

6 nM (IC50)

SGK3

63 nM (IC50)

RSK1

85 nM (IC50)

CHK2

860 nM (IC50)

Aurora B

1840 nM (IC50)

In Vitro

AT13148 inhibits a panel of kinases at 10 μM, and the IC50 values for p70S6K, PKA, ROCKI, and ROCKII are all less than 10 nM and those for AKT1, 2, and 3 are 38, 402, and 50 nM, respectively. For the related AGC kinases RSK1 and SGK3, the IC50 values are 85 and 63 nM, respectively. In contrast, IC50 values for the non-AGC kinases CHK2 and Aurora B are both greater than 800 nM. AT13148 potently inhibits proliferation with GI50 values of 1.5 to 3.8 μM across a selected panel of cancer cell lines[1]. AT13148 treatment in gastric cancer cells dramatically suppresses activation of multiple AGC kinases, including Akt (at p-Thr-308), p70S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK-3β) and p90 ribosomal S6 kinase (RSK)[2].

In Vivo

Oral drug administration of 5 mg/kg of AT13148 results in complete bioavailability. Clear inhibition of phosphorylation of the AKT substrates GSK3β, tuberin, and the p70S6K target S6RP are also observed in PTEN-deficient MES-SA human uterine tumor xenografts after treatment with 40 and 50 mg/kg p.o. of AT13148[1]. Oral gavage of AT13148 at well-tolerated doses significantly inhibits HGC27 xenograft tumor growth in nude mice. AGC activity is also dramatically decreased in AT13148-administrated HGC27 tumors[2].

Clinical Trial
Molecular Weight

313.78

Formula

C₁₇H₁₆ClN₃O

CAS No.

1056901-62-2

SMILES

ClC1=CC=C([[email protected]](C2=CC=C(C3=CNN=C3)C=C2)(O)CN)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (159.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1869 mL 15.9347 mL 31.8695 mL
5 mM 0.6374 mL 3.1869 mL 6.3739 mL
10 mM 0.3187 mL 1.5935 mL 3.1869 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.97 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cells are seeded onto 96-well micro-plates at a density of 1×104 cells per well. After treatment, MTT solution (0.5 mg/mL) is added for 2-3 h. The MTT-purple formazan productions are dissolved in 0.1 N hydrochloric acid, and optical density (OD) is obtained through the micro-plate reader at 570 nm wavelength.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

For pharmacokinetic analysis, male athymic BALB/c mice are obtained from Harlan. AT13148 is formulated in 10% DMSO, 1% Tween-20, and 89% saline and administered at 5 mg/kg i.v. or p.o. Duplicate samples of heparinized whole blood are collected by cardiac puncture at 1, 2, 4, 6, 8, 16, 24, and 72 hours after dosing. Plasma and tissues (liver, kidney, spleen, and muscle are also taken) are prepared and frozen at −20°C until analysis. AT13148 is extracted from plasma and tissues using acetonitrile containing an internal standard and quantified using a liquid chromatography tandem mass spectrometry (LC-MS/MS) method and appropriate standard curves. Pharmacokinetic parameters are determined using WinNonLin software version 5.2.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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AT13148
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