TAI-1

Alias:
Cat No.:V1612 Purity: ≥98%
TAI-1 (TAI 1; TAI1) is a selective Hec1 (High expression in cancer 1) inhibitor with potential anticancer activity.
TAI-1 Chemical Structure CAS No.: 1334921-03-7
Product category: Microtubule Associated
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product 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.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
TAI-1 causes apoptotic cell death, major chromosomal misalignment in metaphase, disruption of the Hec1-Nek2 protein connection, and Nek2 degradation[1]. According to evidence that TAI-1 triggers the activation of apoptotic pathways, it causes cancer cells to die by cleaving the apoptotic proteins Caspase 3 and PARP and degrading the anti-apoptotic protein MCL-1. With GI50 less than 100 nM, TAI-1 is effective against a wide range of cancer cells, including those with chronic myeloid leukemia, cervical cancer, breast cancer, metastatic-pleural, invasive ductal carcinoma, acute myeloid leukemia, myelogenous leukemia, and colorectal carcinoma cells[1].
ln Vivo
In several cancer xenograft models, TAI-1 (20 mg/kg intravenously IV; 150 mg/kg oral PO/BID) suppresses tumor growth[1].
Animal Protocol
Animal/Disease Models: CB-17 SCID (severe combined immunodeficient) mouse (6-7 weeks, 21- 24 g)[1].
Doses: 20 mg/kg intravenously (iv)IV/ or 150 mg/kg per oral PO/BID.
Route of Administration: QDx28 cycles.
Experimental Results: Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models. Did not lead to any loss in body weight.
References
[1]. Lynn Y L Huang, et al. Characterization of the Biological Activity of a Potent Small Molecule Hec1 Inhibitor TAI-1. J Exp Clin Cancer Res. 2014 Jan 9;33(1):6.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H21N3O3S
Molecular Weight
431.51
CAS #
1334921-03-7
SMILES
CC1=C(C(=CC(=C1)OC2=CC=C(C=C2)OC)C)C3=CSC(=N3)NC(=O)C4=CC=NC=C4
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)
Chemical Name
N-[4-[4-(4-Methoxyphenoxy)-2,6-dimethylphenyl]-2-thiazolyl]-4-pyridinecarboxamide
Synonyms

TAI1; TAI 1; TAI-1

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 86 mg/mL (199.3 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3174 mL 11.5872 mL 23.1744 mL
5 mM 0.4635 mL 2.3174 mL 4.6349 mL
10 mM 0.2317 mL 1.1587 mL 2.3174 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Biological Data
  • 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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