2250404-95-4
2250404-95-4 structure
- Name: N-(4-(4-((5-(2-Methoxyethoxy)pyrazin-2-yl)thio)-2,6-dimethylphenyl)thiazol-2-yl)isonicotinamide 4-methylbenzenesulfonate
- Chemical Name: T-1101 tosylate
- CAS Number: 2250404-95-4
- Molecular Formula: C31H31N5O6S3
- Molecular Weight: 665.80
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2020-04-08 17:05:13
- Modify Date: 2025-08-24 20:14:22
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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]
| Name | T-1101 tosylate |
|---|
| 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[1] |
|---|---|
| Related Catalog | |
| Target |
Hec1/Nek2[1] |
| In Vitro | 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 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[1] 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 [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] 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. |
| References |
| Molecular Formula | C31H31N5O6S3 |
|---|---|
| Molecular Weight | 665.80 |