T-1101 tosylate

Research use only, not for human use.

T-1101 tosylate is an inhibitor of Hec1/Nek2 with antitumor activity.

T-1101 tosylate is an inhibitor of Hec1/Nek2 with antitumor activity.(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.

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. Apoptosis Analysis 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 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.

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. Animal Model:SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts 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.

TAI-95 tosylate

Cytoskeleton/Cell Adhesion Molecules

Microtubule/Tubulin

Hec1

——

——

2250404-95-4

665.8

C31H31N5O6S3

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (93.87 mM)

Cc1ccc(cc1)S(O)(=O)=O.COCCOc1cnc(Sc2cc(C)c(-c3csc(NC(=O)c4ccncc4)n3)c(C)c2)cn1

——

(-20℃)

With Ice Pack

≥ 2 years