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    TAI-1
    TAI-1

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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 #: V1612
    CAS #: 1334921-03-7Purity ≥98%

    Description: TAI-1 (TAI 1; TAI1) is a selective Hec1 (High expression in cancer 1) inhibitor with potential anticancer activity. It inhibits the Hec1-Nek2 protein-protein interaction with a GI50 of 13.48 nM in K562 cells, which is >1000-fold higher than that of  INH1 (GI50 =11.7 μM). TAI-1 showed strong anti-proliferative activity in vitro against a broad spectrum of cancer cells. 

    References: J Exp Clin Cancer Res. 2014 Jan 9;33:6.

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    Molecular Weight (MW)431.51
    FormulaC24H21N3O3S
    CAS No.1334921-03-7
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (199.3 mM)
    Water:<1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: N-[4-[4-(4-Methoxyphenoxy)-2,6-dimethylphenyl]-2-thiazolyl]-4-pyridinecarboxamide

    InChi Key: NBNNDUZYMXBCOX-UHFFFAOYSA-N

    InChi Code: InChI=1S/C24H21N3O3S/c1-15-12-20(30-19-6-4-18(29-3)5-7-19)13-16(2)22(15)21-14-31-24(26-21)27-23(28)17-8-10-25-11-9-17/h4-14H,1-3H3,(H,26,27,28)

    SMILES Code: O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(OC4=CC=C(OC)C=C4)C=C3C)=CS2

    Synonyms

    TAI1; TAI 1; TAI-1


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    In Vitro

    In vitro activity: TAI-1 disrupts the binding of Nek2 to Hec1, which leads to degradation of Nek2 and chromosomal misalignment. TAI-1 shows strong growth inhibitory potency at nM levels across a broad spectrum of tumor cells, and produces synergistic activity with doxorubicin, topotecan and paclitaxel in leukemia, breast and liver cancer cells.


    Cell Assay: Cells (MDA-MB-231, MDA-MB-468, K562, HeLa, MCF7, HCC1954, A549, COLO205, U2OS, Huh-7, U937, HepG2, KG-1, PC3, BT474, MV4-11, RS4;11, MOLM-13, WI-38, HUVEC, RPTEC, HAoSMC, MDA-MB-453, T47D, ZR-75-1, ZR-75-30, MDA-MB-361, Hs578T, NCI-H520, Hep3B, PLC/PRF/5, RPMI8226, MOLT-4, N87, MES-SA/Dx5, NCI/ADR-RES, and K562R cells) are seeded in 96 well plates, incubated for 24 hours, compounds added and incubated for 96 hours. All testing points are tested in triplicate wells. Cell viability is determined by MTS assay using CellTiter 96® Aqueous Non-radioactive Cell Proliferation Assay system according to manufacturer’s instructions with MTS and PMS. Data retrieved from spectrophotometer are processed in Excel and GraphPad Prism 5 to calculate the concentration exhibiting 50% growth inhibition (GI50). All data represent the results of triplicate experiments.

    In VivoTAI-1 (20 mg/kg i.v. or 150 mg/kg p.o.) causes significant tumor growth delay in Huh-7 model and modest tumor inhibition in Colo205 and MDA-MB-231 models.
    Animal modelFemale mice bearing Colo-205 or Huh-7 tumors; male mice bearing MDA-MB-231 tumors
    Formulation & DosageDissolved in 10% DMSO 25% PEG200; 5% DMSO, 10% Cremophor, 85% water;  20 mg/kg i.v./QDx28 cycles or 150 mg/kg p.o./BID/28 cycles in total; i.v. or p.o.
    References

    J Exp Clin Cancer Res. 2014 Jan 9;33:6.


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

    TAI-1

    TAI-1 Disrupts Hec1-Nek2 interactions, induces chromosomal misalignment and induces apoptosis of cancer cells. J Exp Clin Cancer Res. 2014 Jan 9;33:6.
     

    TAI-1

    TAI-1 inhibits growth of multiple tumor types in xenografted mouse models. J Exp Clin Cancer Res. 2014 Jan 9;33:6.


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