TAI-1

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TAI-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1334921-03-7
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议

产品介绍

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.

理化性质和储存条件

Molecular Weight (MW)	431.51
Formula	C24H21N3O3S
CAS No.	1334921-03-7
Storage	-20℃ for 3 years in powder form
Storage	-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

实验参考方法

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(R) 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.