TAI-1,98.02%

产品编号:Bellancom-B0790| CAS NO:1334921-03-7| 分子式:C24H21N3O3S| 分子量:431.51

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-B0790
900.00 杭州 北京(现货)
Bellancom-B0790
1500.00 杭州 北京(现货)
Bellancom-B0790
3000.00 杭州 北京(现货)
Bellancom-B0790
4200.00 杭州 北京(现货)
Bellancom-B0790
6200.00 杭州 北京(现货)

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TAI-1

产品介绍 TAI-1 是具有口服活性的、抗肿瘤活性的化合物,是高效的、first-in-class Hec1 抑制剂,在 K562 细胞中的 GI50 值为 13.48 nM。
生物活性

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI50 of 13.48 nM in K562 cells.

体外研究

TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death.
TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways.
TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI50 less than 100 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C.B-17 SCID mice (6-7 weeks, 21-24 g).
Dosage: 20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
Administration: QDx28 cycles.
Result: Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.
Did not lead to any loss in body weight.
体内研究

TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C.B-17 SCID mice (6-7 weeks, 21-24 g).
Dosage: 20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID.
Administration: QDx28 cycles.
Result: Led to significant tumor growth retardation in Huh-7 and modest tumor inhibition was noted tor the Colo205 and MDA-MB-231 models.
Did not lead to any loss in body weight.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (231.74 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3174 mL 11.5872 mL 23.1744 mL
5 mM 0.4635 mL 2.3174 mL 4.6349 mL
10 mM 0.2317 mL 1.1587 mL 2.3174 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。-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    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.79 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.79 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 西域 网站选购。
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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