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    AT13148
    AT13148

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0170
    CAS #: 1056901-62-2Purity ≥98%

    Description: AT13148 is a novel, potent, orally bioavailable, ATP-competitive, multi-AGC kinase inhibitor with potential anticancer activity. It inhibits Akt1/2/3, p70S6K, PKA, and ROCKI/II with IC50 of 38 nM/402 nM/50 nM, 8 nM, 3 nM, and 6 nM/4 nM respectively. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK, and SGK substrate phosphorylation and induced apoptosis in a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects in vitro and in vivo. 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.

    References:Clin Cancer Res. 2012 Jul 15;18(14):3912-23.

    Related CAS #: 1056901-67-7 (R-isomer); 857532-13-9 (racemic)   

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    • 香港大学
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    Molecular Weight (MW)313.78
    FormulaC17H16ClN3O
    CAS No.1056901-62-2
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 62 mg/mL (197.59 mM)
    Water: <1 mg/mL
    Ethanol:  <1 mg/mL
    Other info

    Synonym: AT-13148; AT 13148; AT13148; AT13148 hydrochloride; AT13148 HCl

    InChi Key: IIRWNGPLJQXWFJ-KRWDZBQOSA-N

    InChi Code: InChI=1S/C17H16ClN3O/c18-16-7-5-15(6-8-16)17(22,11-19)14-3-1-12(2-4-14)13-9-20-21-10-13/h1-10,22H,11,19H2,(H,20,21)/t17-/m0/s1

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

    Chemical Name(S)-1-(4-(1H-pyrazol-4-yl)phenyl)-2-amino-1-(4-chlorophenyl)ethanol


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    In Vitro

    Kinase Assay: 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 Assay: Cytotoxicity is determined using a 72 h Alamar Blue assay or a 96 h SRB assay. 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; Incubation Time: 72 hours or 96 hours

    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.

    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.

    Animal model

    Athymic mice bearing MES-SA, BT474, or PC3 tumor xenografts

    Formulation & Dosage

    Dissolved in 10% DMSO, 1% Tween-20, and 89% saline; 50 mg/kg; p.o.

    References

    [1] Yap TA, et al. Clin Cancer Res. 2012, 18(14), 3912-3923.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    AT13148

    The effect of AT13148 exposure on AGC kinase biomarker expression.


    AT13148

    Pharmacodynamic biomarker and antitumor activity of AT13148 in human tumor xenografts. Clin Cancer Res. 2012, 18(14), 3912-3923.

    AT13148

    Comparison of the effects of 6-hour treatment of AT13148 versus CCT128930 on gene and protein expression in U87MG human glioblastoma cells


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