2. Cell Cycle/DNA Damage Apoptosis
  3. NEKs Apoptosis
  4. TAI-1

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.

For research use only. We do not sell to patients.

TAI-1 Chemical Structure

TAI-1 Chemical Structure

CAS No. : 1334921-03-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
25 mg USD 300 In-stock
50 mg USD 420 In-stock
100 mg USD 620 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

TAI-1 Related Antibodies

Top Publications Citing Use of Products

View All NEKs Isoform Specific Products:

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NEK1 NEK2 NEK6 NEK7

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

 

Cellular Effect
Cell Line Type Value Description References
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]
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]
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]
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]
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-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-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]
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]
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.

TAI-1 Related Antibodies
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.
Molecular Weight

431.51

Formula

C24H21N3O3S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TAI-11334921-03-7TAI1TAI 1NEKsApoptosisNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesInhibitorinhibitorinhibit

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