TAI-1

Catalog No.S7495 Batch:S749501

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Technical Data

Formula

C24H21N3O3S
Molecular Weight 431.51 CAS No. 1334921-03-7
Solubility (25°C)* In vitro DMSO 86 mg/mL (199.3 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.
Targets
Hec1 [1]
In vitro 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. [1]
In vivo TAI-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. [1]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    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

  • Concentrations

    ~10 μM

  • Incubation Time

    96 hours

  • Method

    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.
Animal Study:[1]
  • Animal Models

    Female mice bearing Colo-205 or Huh-7 tumors; male mice bearing MDA-MB-231 tumors

  • Dosages

    20 mg/kg i.v./QDx28 cycles or 150 mg/kg p.o./BID/28 cycles in total

  • Administration

    i.v. or p.o.

Selleck's TAI-1 has been cited by 3 publications

Nek2 Augments Sorafenib Resistance by Regulating the Ubiquitination and Localization of β-catenin in Hepatocellular Carcinoma [ J Exp Clin Cancer Res, 2019, 18;38(1):316] PubMed: 31319849
Centromere Dysfunction Compromises Mitotic Spindle Pole Integrity [ Curr Biol, 2019, 29(18):3072-3080.e5] PubMed: 31495582
Centromere Dysfunction Compromises Mitotic Spindle Pole Integrity. [ Curr Biol, 2019, 29(18):3072-3080] PubMed: 31495582

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.