| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S88429-1mg买3赠1 |
99.30% | ￥280.00 |
6 | - | - | - | - |
|
S88429-5mg买3赠1 |
99.30% | ￥720.00 |
9 | - | - | - | - |
|
S88429-10mg买3赠1 |
99.30% | ￥1200.00 |
9 | - | - | - | - |
|
S88429-25mg买3赠1 |
99.30% | ￥2000.00 |
1 | - | - | - | - |
|
S88429-50mg买3赠1 |
≥98% | ￥3200.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | IACS-010759 is an orally bioavailable inhibitor of complex I of oxidative phosphorylation of the mitochondrial electron transport chain | ||||||||||||||||||||
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| 靶点： | Apoptosis;Mitochondrial Metabolism;Apoptosis; Others; MitochondrialMetabolism | ||||||||||||||||||||
| 体内研究： | In mice following intravenous (0.3mg per kg body weight (mg/kg)) and oral (1mg/kg) administration, IACS-010759 was characterized by low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24h) of IACS-010759 with sustained levels of compound in the plasma following oral dosing. Treatment with IACS-010759 at the 5 or 10mg/kg dose resulted in tumor regression with minimal body weight loss, whereas IACS-010759 at the 25mg/kg dose was not tolerated, and body weight loss, lethargy, and hypothermia were observed | ||||||||||||||||||||
| 细胞实验： | CLL cells were incubated with either dimethyl sulfoxide (control) or IACS-010759 (100 nM) for 24 h. A total of 10^6 cells were stained with MitoSOX Red and tetramethylrhodamine ethyl ester perchlorate and were analyzed using flow cytometry for mitochondrial reactive oxygen species (ROS) and mitochondrial outer membrane potential, respectively | ||||||||||||||||||||
| 动物实验： | OCI-AML3 cells were expanded in RPMI medium + 5% or 10% fetal bovine serum (FBS) until ≥150 million cells were present. For OCI-AML3, 2 million cells in 200 μl of saline were injection into the tail vein of NSG mice. For the patient-derived models, 4030094 and S6-AP, cells were harvested from mice with advanced disease or resuscitated from frozen vials, washed and resuspended at 5 x 10^6 cells/ml in PBS. Mice were irradiated for 24 hours at 250 cGY before orthotopic implantation of 1 x 10^6 cells suspended in 200 μl of saline were into the tail vein of 6- to 8-week old female NSG mice. For OCI-AML3, treatment began when whole body luminescence averaged 5 x 10^7. For model 4030094, treatment for the efficacy began when animals reached 10% burden and for the PK/PD studies when the animals reached 80% disease burden as measured by human and mouse CD45 and viability (DAPI 62248) staining followed by flow cytometry with a Fortessa flow cytometer. Mice were randomized based on luminescence for the OCI-AML3 model an | ||||||||||||||||||||
| 参考文献： | 1. Lissanu Deribe Y, et al. Mutations in the SWI/SNF complex induce a targetable dependence on oxidative phosphorylation in lung cancer. Nat Med. 2018 Jul;24(7):1047-1057. 2. Molina JR, et al. An inhibitor of oxidative phosphorylation exploits cancer vulnerability. Nat Med. 2018 Jul;24(7):1036-1046. 3. Vangapandu HV, et al. Biological and metabolic effects of IACS-2010759, an OxPhos inhibitor, on chronic lymphocytic leukemia cells. Oncotarget. 2018 May 18;9(38):24980-241991. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京