2. Cell Cycle/DNA Damage Apoptosis
  3. NEKs Apoptosis
  4. T-1101 tosylate

T-1101 tosylate  (Synonyms: TAI-95 tosylate)

Cat. No.: HY-120356A Purity: 99.05%
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T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models.

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T-1101 tosylate Chemical Structure

T-1101 tosylate Chemical Structure

CAS No. : 2250404-95-4

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Based on 1 publication(s) in Google Scholar

Other Forms of T-1101 tosylate:

T-1101 tosylate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE T-1101 tosylate

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NEK1 NEK2 NEK6 NEK7

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Description

T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models[1].

IC50 & Target

NEK2

 

In Vitro

T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM)[2].
T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells[2].
T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner[2].
T-1101 tosylate (1 μM; 24 hours) induces apoptosis[2].
T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1[2].

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

T-1101 tosylate Related Antibodies

Apoptosis Analysis[2]

Cell Line: HeLa cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: Increased the amount of apoptotic marker proteins cleaved caspase-3 and PARP and decreased the amount of antiapoptotic proteins Mcl-1 and XIAP in HeLa cells.

Western Blot Analysis[2]

Cell Line: K562 cells
Concentration: 1 μM
Incubation Time: 3 hours, 6 hours, 16 hours, 24 hours
Result: Lowered the level of Nek2 in a time-dependent manner.
In Vivo

T-1101 tosylate shows good oral bioavailability and thermal stability [2].
Oral co-administration of T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) halves the dose of sorafenib (25 mg/kg to 12.5 mg/kg) required to exhibit comparable in vivo activity towards Huh-7 xenografts [2].
T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts[2].

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

Animal Model: SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts[2]
Dosage: 25 mg/kg, 50 mg/kg
Administration: Oral administration; twice per day; 28 days
Result: Showed significant in vivo activity in mice bearing various human cancer xenografts.
Clinical Trial
Molecular Weight

665.80

Formula

C31H31N5O6S3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=CC(SC2=NC=C(OCCOC)N=C2)=CC(C)=C1C3=CSC(NC(C4=CC=NC=C4)=O)=N3.CC(C=C5)=CC=C5S(=O)(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (93.87 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 1.5020 mL 7.5098 mL 15.0195 mL
5 mM 0.3004 mL 1.5020 mL 3.0039 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
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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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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 1.5020 mL 7.5098 mL 15.0195 mL 37.5488 mL
5 mM 0.3004 mL 1.5020 mL 3.0039 mL 7.5098 mL
10 mM 0.1502 mL 0.7510 mL 1.5020 mL 3.7549 mL
15 mM 0.1001 mL 0.5007 mL 1.0013 mL 2.5033 mL
20 mM 0.0751 mL 0.3755 mL 0.7510 mL 1.8774 mL
25 mM 0.0601 mL 0.3004 mL 0.6008 mL 1.5020 mL
30 mM 0.0501 mL 0.2503 mL 0.5007 mL 1.2516 mL
40 mM 0.0375 mL 0.1877 mL 0.3755 mL 0.9387 mL
50 mM 0.0300 mL 0.1502 mL 0.3004 mL 0.7510 mL
60 mM 0.0250 mL 0.1252 mL 0.2503 mL 0.6258 mL
80 mM 0.0188 mL 0.0939 mL 0.1877 mL 0.4694 mL
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T-1101 tosylate 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:

T-11012250404-95-4TAI-95T1101T 1101TAI95TAI 95NEKsApoptosisNIMA–related KinasesNIMA (never in mitosis gene a)-related Expressed KinasesHec1/Nek2PPIInhibitorinhibitorinhibit

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