Art. -Nr.: HY-B0790

TAI-1

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TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI₅₀ of 13.48 nM in K562 cells.

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Reinheit: 98.60%
CAS. Nr.: 1334921-03-7
Formel: C₂₄H₂₁N₃O₃S
Molecular Weight:431.51

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

TAI-1 Chemical Structure

CAS. Nr.: 1334921-03-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI₅₀ of 13.48 nM in K562 cells^[1].

IC₅₀ & Target

NEK2

Alle NEKs Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	48.6 nM Compound: 31	Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay Antiproliferative activity against human HeLa cells assessed as cell viability after 96 hrs by CellTiter96 assay	[PMID: 24773549]
HeLa	IC₅₀	48.6 nM Compound: 7	Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay Antiproliferative activity against human HeLa cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay	[PMID: 32113126]
K562	IC₅₀	34.9 nM Compound: 31	Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay Antiproliferative activity against human K562 cells assessed as cell viability after 96 hrs by CellTiter96 assay	[PMID: 24773549]
K562	IC₅₀	34.9 nM Compound: 7	Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay Antiproliferative activity against human K562 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay	[PMID: 32113126]
MDA-MB-231	IC₅₀	32 nM Compound: 31	Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 96 hrs by CellTiter96 assay	[PMID: 24773549]
MDA-MB-231	IC₅₀	32 nM Compound: 7	Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay Antiproliferative activity against human MDA-MB-231 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay	[PMID: 32113126]
MDA-MB-468	IC₅₀	37 nM Compound: 31	Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay Antiproliferative activity against human MDA-MB-468 cells assessed as cell viability after 96 hrs by CellTiter96 assay	[PMID: 24773549]
MDA-MB-468	IC₅₀	37 nM Compound: 7	Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay Antiproliferative activity against human MDA-MB-468 cells measured after 96 hrs by CellTiter 96 Aqueous One Solution Reagent based assay	[PMID: 32113126]

In Vitro

TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death^[1].
TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways^[1].
TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI₅₀ less than 100 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

C.B-17 SCID mice (6-7 weeks, 21-24 g)^[1].
Dosage:

20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
Administration:

QDx28 cycles.
Result:

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.

Chemical Information

CAS. Nr. 1334921-03-7
Appearance Solid
Molecular Weight 431.51
Formel C₂₄H₂₁N₃O₃S
Color White to off-white
SMILES

O=C(C1=CC=NC=C1)NC2=NC(C3=C(C)C=C(OC4=CC=C(OC)C=C4)C=C3C)=CS2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (231.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3174 mL	11.5872 mL	23.1744 mL	57.9361 mL
	5 mM	0.4635 mL	2.3174 mL	4.6349 mL	11.5872 mL
	10 mM	0.2317 mL	1.1587 mL	2.3174 mL	5.7936 mL
	15 mM	0.1545 mL	0.7725 mL	1.5450 mL	3.8624 mL
	20 mM	0.1159 mL	0.5794 mL	1.1587 mL	2.8968 mL
	25 mM	0.0927 mL	0.4635 mL	0.9270 mL	2.3174 mL
	30 mM	0.0772 mL	0.3862 mL	0.7725 mL	1.9312 mL
	40 mM	0.0579 mL	0.2897 mL	0.5794 mL	1.4484 mL
	50 mM	0.0463 mL	0.2317 mL	0.4635 mL	1.1587 mL
	60 mM	0.0386 mL	0.1931 mL	0.3862 mL	0.9656 mL
	80 mM	0.0290 mL	0.1448 mL	0.2897 mL	0.7242 mL
	100 mM	0.0232 mL	0.1159 mL	0.2317 mL	0.5794 mL

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TAI-1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle NEKs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TAI-1

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Orally Active Compound Library

Anti-Blood Cancer Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle NEKs Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

TAI-1 Related Classifications

HY-B0790 Related Classifications