TAI-1

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

TAI-1 

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。

TAI-1

TAI-1 Chemical Structure

CAS No. : 1334921-03-7

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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[1].

IC50 & Target

GI50: 13.48 nM (in K562 cells)[1].

体外研究
(In Vitro)

TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death[1].
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[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd 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)[1].
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.

分子量

431.51

Formula

C24H21N3O3S

CAS 号

1334921-03-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Lynn Y L Huang, et al. Characterization of the Biological Activity of a Potent Small Molecule Hec1 Inhibitor TAI-1. J Exp Clin Cancer Res. 2014 Jan 9;33(1):6.

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