1. Apoptosis
  2. Apoptosis
  3. T-1101 tosylate

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

目录号: HY-120356A
产品使用指南

T-1101 tosylate (TAI-95 tosylate) 是一种具有抗肿瘤活性的 Hec1/Nek2 抑制剂。T-1101 tosylate 对正常细胞、激酶和 hERG 无抑制效果。

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T-1101 tosylate Chemical Structure

T-1101 tosylate Chemical Structure

CAS No. : 2250404-95-4

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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]

IC50 & 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.
Molecular Weight

665.80

Formula

C₃₁H₃₁N₅O₆S₃

CAS No.

2250404-95-4

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

T-1101TAI-95T1101T 1101TAI95TAI 95ApoptosisHec1/Nek2PPIInhibitorinhibitorinhibit

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T-1101 tosylate
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HY-120356A
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