| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 25mg | 询价 |
| 50mg | 询价 |
Birinapant (TL32711) is a SMAC mimetic designed to specifically target cIAP1 and cIAP2 for degradation.
Preparation Method | A fluorescence polarization assay was used to determine the dissociation constants (K d) of Smac mimetics Birinapant (TL32711) and GT13402 for XIAP and cIAP1 by monitoring the decrease in fluorescence polarization signal due to competitive displacement of an FP peptide from the BIR3/FP peptide binary complex. |
Applications | The binding constants (K d) of Birinapant (TL32711) for XIAP and cIAP1 were determined to be 45 and |
Cell lines | 451Lu and WM1366 melanoma cells |
Preparation Method | Cells were treated with Birinapant (TL32711) 1 μmol/L in combination with TNF-α 1 ng/mL. Cells were then incubated for 72 hours in the presence or absence of Necrostatin-1 a RIP1 kinase inhibitor. Proliferation was assessed using the MTS assay. |
Reaction Conditions | 1 μmol/L Birinapant (TL32711) for 72 hours |
Applications | The majority of cell lines exhibited strong combination activity of Birinapant (TL32711) and TNF-α. |
Animal models | Male C57BL/6J mice aged 8 week old, weighing 21 ± 1.3g |
Preparation Method | Before the LPS administration, mice were injected intraperitoneally with Birinapant (TL32711) (30 mg/kg body weight, Birinapant (TL32711) group) either vehicle control (vehicle group) for 24 h. Birinapant (TL32711) was dissolved in 12.5% Captisol in distilled water. Twenty-four mice in each group were euthanized and the samples of the liver and blood were harvested at 0, 6, 12 and 24 h after LPS challleage. |
Dosage form | 30 mg/kg Birinapant (TL32711) ip. for 24 h. |
Applications | Birinapant (TL32711) pretreatment significantly improved mice survival. |
| 产品描述 | Birinapant (TL32711) is a SMAC mimetic designed to specifically target cIAP1 and cIAP2 for degradation[1]. the binding constants (K d) of Birinapant (TL32711) for XIAP and cIAP1 were determined to be 45 and[3]. When Birinapant (TL32711) was combined with TNF-α, strong combination activity, that is, neither compound was effective individually but the combination was highly effective, was observed in 12 of 18 cell lines.Birinapant (TL32711) combined with TNF-α inhibited the growth of a melanoma cell line with acquired resistance to BRAF inhibition to the same extent as in the parental cell line[1]. When investigated the role of Birinapant (TL32711) in radiosensitization of glioblastoma cells, Birinapant (TL32711) can enhance the radiosensitivity of glioblastoma cell lines in cell-based assays and tumor models via radiation-induced TNF-α[4]. Combination of Birinapant (TL32711) and TNFα induced sub-G0 DNA fragmentation in sensitive lines and Birinapant (TL32711) alone also induced significant G2-M cell-cycle arrest and cell death in UM-SCC-46 cells[6]. Birinapant (TL32711) induced death receptor-/caspase-8-mediated apoptosis in AML cells, including in AML stem/progenitor cells, but not in normal CD34(+) cells[7]. Birinapant (TL32711) significantly improved the survival rate of endotoxemic mice and attenuated LPS-induced liver pathologic damage and inflammatory response. IL-1 and TNF-α levels in the serum were markedly decreased in Birinapant (TL32711) pretreatment mice compared with control mice .The cellular inhibitor of apoptosis protein 1 (cIAP1) expression in liver resident macrophage (Kupffer cells, KCs) was significantly decreased in the Birinapant (TL32711) group compared to the Vehicle group[2]. References: |
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