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| 产品名称 | p53 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Pifithrin-μ | ✔ | 99%+ | |||||||||||||||||
| Pifithrin-α HBr | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | JNJ-26854165 is a p53-activating agent which can induce p53-mediated apoptosis in acute leukemia cells with wild-type p53, in which p53 rapidly drives transcription-independent apoptosis followed by activation of a transcription-dependent pathway. It accelerated the proteasome-mediated degradation of p21 and antagonized the transcriptional induction of p21 by p53[3]. The action of JNJ-26854165 relies on HDM2, a key regulator of p53, mediating its rapid degradation. It is regarded as a first-in-class HDM2-inhibitor in phase I development[2]. |
| Concentration | Treated Time | Description | References | |
| 293T cells | 5 µM | 24 hours | Observed accumulation of cholesterol within endosomes | J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. |
| U87 cells | 10 µM | Detected VEGF promoter activity, found Serdemetan reduced VEGF levels | PLoS One. 2013 Sep 6;8(9):e74741. | |
| U373 cells | 10 µM | 6 hours | Detected p53 and p21 levels, found Serdemetan did not significantly induce p21 | PLoS One. 2013 Sep 6;8(9):e74741. |
| SF767 cells | 10 µM | 6 hours | Detected p53 and p21 levels, found Serdemetan did not significantly induce p21 | PLoS One. 2013 Sep 6;8(9):e74741. |
| U87MG cells | 30 µM | 6 hours | Detected p53 and Mdm2 levels, found Serdemetan increased p53 levels but did not robustly induce Mdm2 | PLoS One. 2013 Sep 6;8(9):e74741. |
| MM cells | 1.43-2.48 µM (IC50) | 72 hours | Evaluated proliferation inhibition, showing dose-dependent inhibition | J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. |
| MCL cells | 0.25-3 µM (IC50) | 72 hours | Evaluated proliferation inhibition, showing dose-dependent inhibition | J Pharmacol Exp Ther. 2013 Sep;346(3):381-92. |
| Dose | Mice: 20 mg/kg[3] (p.o.), 50 mg/kg[4] (p.o.) |
| Administration | p.o. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00676910 | Neoplasms | Phase 1 | Completed | - | - |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
3.04mL 0.61mL 0.30mL |
15.22mL 3.04mL 1.52mL |
30.45mL 6.09mL 3.04mL |
|
| CAS号 | 881202-45-5 |
| 分子式 | C21H20N4 |
| 分子量 | 328.41 |
| SMILES Code | C(CC1=CNC2=C1C=CC=C2)NC1=CC=C(NC2=CC=NC=C2)C=C1 |
| MDL No. | MFCD16620518 |
| 别名 | JNJ-26854165 |
| 运输 | 蓝冰 |
| InChI Key | CEGSUKYESLWKJP-UHFFFAOYSA-N |
| Pubchem ID | 11609586 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
| 溶解方案 |
DMSO: 50 mg/mL(152.25 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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