产品
编 号:F123719
分子式:C24H21N3O3S
分子量:431.51
产品类型
结构图
CAS No: 1334921-03-7
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产品详情
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.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.