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Gamitrinib TPP
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gamitrinib TPP图片
CAS NO:1131626-46-4
包装:5 mg
市场价:7000元

产品介绍

产品描述

Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity. Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor.

体外活性

Within a 16-hour exposure, concentrations of Gamitrinib TPP of 15-20 μM indistinguishably kill patient-derived and cultured glioblastoma cell lines.?This cell death response has the hallmarks of mitochondrial apoptosis, with loss of organelle inner membrane potential, release of cytochrome c in the cytosol, activation of initiator caspase-9 and effector caspase-3 and -7, and cellular reactivity for annexin V. Because Hsp90s are selectively present in mitochondria of tumor cells, but not normal tissues, Gamitrinib TPP does not kill normal fetal human astrocytes (FHAS).?Under comparable conditions, nonsubcellularly targeted 17-AAG has no effect on normal or tumor cells.

体内活性

2 cycles of intracranial TRAIL combined with systemic G-TPP suppress the growth of established glioblastomas, with no significant animal weight loss throughout treatment.?Analysis of brain sections from these mice, but not single agent-treated animals, show loss of tumor cell proliferation, internucleosomal DNA fragmentation, and caspase-3 activity, consistent with extensive activation of apoptosis in vivo.

Cas No.

1131626-46-4

分子式

C52H65N3O8P

分子量

891.06

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years