Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gamitrinib TPP hexafluorophosphate is a potent HSP90 inhibitor that specifically targets the mitochondria, demonstrating notable anti-cancer activity. It functions by inhibiting the mitochondrial matrix, making it an effective compound in cancer treatment.
产品描述 | Gamitrinib TPP hexafluorophosphate is a potent HSP90 inhibitor that specifically targets the mitochondria, demonstrating notable anti-cancer activity. It functions by inhibiting the mitochondrial matrix, making it an effective compound in cancer treatment. |
体外活性 | Gamitrinib TPP is selectively delivered to mitochondria and does not affect Hsp90 homeostasis outside the organelle. 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 caspase-7, and cellular reactivity for annexin V.Gamitrinib TPP (GamitrinibTPP, G-TPP), a small molecule that combines the Hsp90 ATPase inhibitory module of 17-allylamino geldanamycin (17-AAG) with the mitochondrial-targeting moiety of triphenylphosphonium. |
体内活性 | Whether the combination of TRAIL plus Gamitrinib TPP (GamitrinibTPP, G-TPP) has activity against glioblastoma in vivo is studied.??systemic monotherapy with Gamitrinib TPP at concentrations (20 mg/kg as daily i.p. injections) that inhibit subcutaneous xenograft tumor growth in mice has no effect on orthotopic glioblastoma growth.Luciferase-expressing U87 glioblastoma cells implanted in the right cerebral striatum of immunocompromised mice give rise to rapidly growing tumors by bioluminescence imaging, and treatment of these mice with vehicle, stereotactic delivery of TRAIL, or systemic administration of suboptimal concentrations of Gamitrinib TPP does not affect tumor growth in vivo.??In contrast, 2 cycles of intracranial TRAIL combined with systemic Gamitrinib TPP suppresses the growth of established glioblastomas, with no significant animal weight loss throughout treatment. |
分子量 | 1036.043 |
分子式 | C52H65F6N3O8P2 |
CAS No. | 1131626-47-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (48.26 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 0.9652 mL | 4.8261 mL | 9.6521 mL | 24.1303 mL |
5 mM | 0.193 mL | 0.9652 mL | 1.9304 mL | 4.8261 mL | |
10 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.413 mL | |
20 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Gamitrinib TPP hexafluorophosphate 1131626-47-5 Cytoskeletal Signaling Metabolism HSP Inhibitor inhibitor inhibit