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

Catalog No.GC61311

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG

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T-1101 tosylate Chemical Structure

Cas No.: 2250404-95-4

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5mg
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10mg
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50mg
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100mg
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

T-1101 tosylate (TAI-95 tosylate) is a Hec1/Nek2 (Highly expressed in cancer 1 / NIMA-related kinase 2) inhibitor with antitumor activity. T-1101 tosylate is inactive toward normal cells, kinases and hERG[1]

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

T-1101 tosylate shows good oral bioavailability and thermal stability [1].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 [1].T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts[1]. Animal Model: SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts[1]

[1]. 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.

Chemical Properties

Cas No. 2250404-95-4 SDF
Synonyms TAI-95 tosylate
Canonical 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
Formula C31H31N5O6S3 M.Wt 665.8
Solubility DMSO: 62.5 mg/mL (93.87 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 1.502 mL 7.5098 mL 15.0195 mL
5 mM 0.3004 mL 1.502 mL 3.0039 mL
10 mM 0.1502 mL 0.751 mL 1.502 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 27 reference(s) in Google Scholar.)

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