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

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T-1101 tosylate (Synonyms: TAI-95 tosylate) 纯度: 99.61%

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。

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

T-1101 tosylate Chemical Structure

CAS No. : 2250404-95-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥6590 In-stock
5 mg ￥4500 In-stock
10 mg ￥7500 In-stock
50 mg 询价
100 mg 询价

* Please select Quantity before adding items.

T-1101 tosylate 相关产品

•相关化合物库:

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  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
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生物活性

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]
体外研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

分子量

665.80

Formula

C31H31N5O6S3
CAS 号

2250404-95-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

DMSO : 62.5 mg/mL (93.87 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5020 mL 7.5098 mL 15.0195 mL
5 mM 0.3004 mL 1.5020 mL 3.0039 mL
10 mM 0.1502 mL 0.7510 mL 1.5020 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.12 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.12 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. 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.

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