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AT13148

رقم الكتالوجGC17712

AT13148 هو مثبط كيناز متعدد AGC نشط شفويًا وتنافسي ATP مع IC50s من 38 نانومتر / 402 نانومتر / 50 نانومتر ، 8 نانومتر ، 3 نانومتر ، 6 نانومتر / 4 نانومتر لـ Akt1 / 2/3 ، p70S6K ، PKA ، و ROCKI / II ، على التوالي

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AT13148 التركيب الكيميائي

Cas No.: 1056901-62-2

الحجم السعر المخزون الكميّة
5mg
71٫00
متوفر
10mg
111٫00
متوفر
50mg
322٫00
متوفر
100mg
460٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of AT13148

AT13148 is a novel, oral and ATP-competitive inhibitor of multi-AGC Kinase with IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM for AKT, p70S6 kinase, PKA, SGK and Rho kinase, respectively [1].

In vitro studies, AT13148 has been reported to inhibit activity of AGC kinases which including AKT, p70S6 kinase, PKA, SGK and Rho kinase with the IC50 values of 38nM, 8nM, 3nM, 63nM and 4nM, respectively. In addition, AT13148 has been revealed to inhibit proliferation with GI50 values of 1.54μM, 1.59μM, 1.82μM, 2.65μM and 3.77μM in MES-SA, BT474, HCT-116, A549 and SK-OV-3 cell lines, respectively.

In vivo studies, AT13148 has shown the antitumor activity in multiple human tumor xenograft models including PTEN-deficient MES-SA human uterine sarcoma, HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts [1].

References:
[1] Yap TA1, Walton MI, Grimshaw KM, Te Poele RH, Eve PD, Valenti MR, de Haven Brandon AK, Martins V, Zetterlund A, Heaton SP, Heinzmann K, Jones PS, Feltell RE, Reule M, Woodhead SJ, Davies TG, Lyons JF, Raynaud FI, Eccles SA, Workman P, Thompson NT, Garrett MD. AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.

Protocol of AT13148

Kinase experiment:

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 experiment:

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.

Animal experiment:

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.

References:

[1]. Yap TA, et al. AT13148 is a novel, oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity. Clin Cancer Res. 2012 Jul 15;18(14):3912-23.
[2]. Xi Y, et al. AT13148, a first-in-class multi-AGC kinase inhibitor, potently inhibits gastric cancer cells both in vitro and in vivo. Biochem Biophys Res Commun. 2016 Sep 9;478(1):330-6.

Chemical Properties of AT13148

Cas No. 1056901-62-2 SDF
Canonical SMILES ClC1=CC=C(C=C1)[C@@](C2=CC=C(C3=CNN=C3)C=C2)(CN)O
Formula C17H16ClN3O M.Wt 313.78
الذوبان DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of AT13148

Prepare stock solution
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
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In vivo Formulation Calculator (Clear solution) of AT13148

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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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