Description
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
Product information
CAS Number: 2250404-95-4
Molecular Weight: 665.80
Formula: C31H31N5O6S3
Chemical Name: 4-methylbenzene-1-sulfonic acid; N-[4-(4-{[5-(2-methoxyethoxy)pyrazin-2-yl]sulfanyl}-2,6-dimethylphenyl)-1,3-thiazol-2-yl]pyridine-4-carboxamide
Smiles: COCCOC1=CN=C(C=N1)SC1=CC(C)=C(C2=CSC(NC(=O)C3C=CN=CC=3)=N2)C(C)=C1.CC1C=CC(=CC=1)S(O)(=O)=O
InChiKey: OUJWEAVKLYQREM-UHFFFAOYSA-N
InChi: InChI=1S/C24H23N5O3S2.C7H8O3S/c1-15-10-18(34-21-13-26-20(12-27-21)32-9-8-31-3)11-16(2)22(15)19-14-33-24(28-19)29-23(30)17-4-6-25-7-5-17;1-6-2-4-7(5-3-6)11(8,9)10/h4-7,10-14H,8-9H2,1-3H3,(H,28,29,30);2-5H,1H3,(H,8,9,10)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (93.87 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
T-1101 tosylate shows potent in vitro antiproliferative activity (IC50: 14.8-21.5 nM). T-1101 tosylate disrupts the Hec1/Nek2 protein–protein interaction in the cells. T-1101 tosylate (1μM; 3-24 24 hours) decreases the level of Nek2 in a time-dependent manner. T-1101 tosylate (1 µM; 24 hours) induces apoptosis. T-1101 tosylate reduces amounts of cell-cycle related proteins cyclin A1, cyclin B1, and cyclin D1.
In Vivo:
T-1101 tosylate shows good oral bioavailability and thermal stability . 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 . T-1101 tosylate (2.5 mg/kg; p.o.; twice per day) shows significant in vivo activity in mice bearing various human cancer xenografts.
Products are for research use only. Not for human use.
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