TAI-1

Catalog No.S7495 Batch:S749502

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

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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

In vitro

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

In Vivo

TAI-1 (20 mg/kg i.v. or 150 mg/kg p.o.) causes significant tumour growth delay in Huh-7 model and modest tumour inhibition in Colo205 and MDA-MB-231 models.

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, this compound 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.

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, this compound 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.

References

https://pubmed.ncbi.nlm.nih.gov/24401611/

Sellecks 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
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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.