| Identification | Back Directory | [Name]
TAI-95 tosylate | [CAS]
2250404-95-4 | [Synonyms]
TAI-95 tosylate
T-1101 tosylate (TAI-95 tosylate)
TAI95,T1101 tosylate,TAI-95,T1101,Apoptosis,Inhibitor,inhibit,T 1101,T-1101,PPI,TAI 95,Hec1/Nek2,T 1101 tosylate
N-(4-(4-((5-(2-Methoxyethoxy)pyrazin-2-yl)thio
)-2,6-dimethylphenyl)thiazol-2-yl)isonicotinami
de 4-methylbenzenesulfonate | [Molecular Formula]
C31H31N5O6S3 | [MOL File]
2250404-95-4.mol | [Molecular Weight]
665.8 |
| Hazard Information | Back Directory | [Uses]
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[1]. | [in vivo]
T-1101 tosylate shows good oral bioavailability and thermal stability [2].
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].
| Animal Model: | SCID mice bearing human Huh-7, BT-474, MCF-7, and MDA-MB-231 xenografts[2] | | 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. |
| [IC 50]
NEK2 | [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. DOI:10.1007/s00280-014-2540-7
[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. DOI:10.1016/j.ejmech.2020.112118 |
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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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