| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S80242-1mg促销 |
99.00% | ￥168.00 ￥134.00 |
6 | - | - | - | - |
|
S80242-5mg促销 |
99.00% | ￥320.00 ￥256.00 |
5 | - | - | - | - |
|
S80242-10mg促销 |
99.00% | ￥416.00 ￥332.00 |
3 | - | - | - | - |
|
S80242-25mg促销 |
99.00% | ￥760.00 ￥608.00 |
4 | - | - | - | - |
|
S80242-50mg促销 |
99.00% | ￥1040.00 ￥832.00 |
4 | - | - | - | - |
|
S80242-100mg促销 |
99.00% | ￥1520.00 ￥1216.00 |
5 | - | - | - | - |
|
S80242-500mg促销 |
99.00% | ￥4800.00 ￥3840.00 |
5 | - | - | - | - |
|
| 产品描述： | (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy | ||||||||||||||||||||
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| 靶点： | IC50: 77/33 nM (BRD4(1/2));EpigeneticReaderDomain;Autophagy;LigandsforTargetProteinforPROTAC | ||||||||||||||||||||
| 体内研究： | Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL) | ||||||||||||||||||||
| 参考文献： | 1. Filippakopoulos P, et al. Selective inhibition of BET bromodomains. Nature. 2010 Dec 23;468(7327):1067-73. 2. Sakamaki JI, et al. Bromodomain Protein BRD4 Is a Transcriptional Repressor of Autophagy and LysosomalFunction. Mol Cell. 2017 May 18;66(4):517-532.e9. 3. Matzuk MM, et al. Small-molecule inhibition of BRDT for male contraception. Cell. 2012 Aug 17;150(4):673-84. | ||||||||||||||||||||
| 溶解性： | DMSO : ≥ 45 mg/mL (98.47 mM) | ||||||||||||||||||||
| 保存条件： | 2-8℃ | ||||||||||||||||||||
| 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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