product name TAI-1
Description: TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction. TAI-1 has a GI50 of 13.48 nM (K562 cells), which is close to 1000 times improvement in potency compared to INH1 (GI50 =11.7 μM). TAI-1 showed strong inhibition across a broad spectrum of tumor cells. TAI-1 interrupted Hec1-Nek2 protein interaction, led to Nek2 degradation, induced significant chromosomal misalignment in metaphase, and induced apoptotic cell death.
References: J Exp Clin Cancer Res. 2014 Jan 9;33:6.
431.51
Formula
C24H21N3O3S
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
Solubility (In vivo)
Synonyms
other peoduct :
| 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. Kinase Assay: 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 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. |
| Animal model | Female mice bearing Colo-205 or Huh-7 tumors; male mice bearing MDA-MB-231 tumors |
| Formulation & Dosage | Dissolved 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. |
