T-1101 tosylate
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.91%
- CAS No.: 2250404-95-4
- Formula: C31H31N5O6S3
- Molecular Weight:665.80
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
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Publications Citing Use of MedChemExpress (MCE) T-1101 tosylate
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Biological Activity
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NEK2 |
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.
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Cell Line:HeLa cells
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Concentration:1 µM
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Incubation Time:24 hours
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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.
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Cell Line:K562 cells
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Concentration:1 μM
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Incubation Time:3 hours, 6 hours, 16 hours, 24 hours
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Result:Lowered the level of Nek2 in a time-dependent manner.
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.
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Animal Model:SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts[2]
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Dosage:25 mg/kg, 50 mg/kg
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Administration:Oral administration; twice per day; 28 days
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Result:Showed significant in vivo activity in mice bearing various human cancer xenografts.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2250404-95-4
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Appearance Solid
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Molecular Weight 665.80
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Formula C31H31N5O6S3
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Color Light yellow to yellow
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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
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Synonyms
TAI-95 tosylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cancer Res Commun
Inhibition of NEK2 Promotes Chemosensitivity and Reduces KSHV-positive Primary Effusion Lymphoma Burden. [Abstract]2024 Apr 9;4(4):1024-1040. PMID: 38592451
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (275 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Huang LY, et al., Inhibition of Hec1 as a novel approach for treatment of primary liver cancer. Cancer Chemother Pharmacol. 2014 Sep;74(3):511-20. [Content Brief]
[2]. Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118. [Content Brief]
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 |
T-1101 tosylate Related Classifications
HY-120356A Related Classifications
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