PAC-1是首个Caspase活化化合物,EC50值为0.22uM,能增强procaspase-3活性并诱导多种癌细胞和小鼠肿瘤模型凋亡。
PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.
~100 μM
~100 mg/kg颗粒皮下移植或口服处理
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Putt KS, et al. Nat Chem Biol, 2006, 2(10), 543-550.
分子式 C23H28N4O2 |
分子量 392.49 |
CAS号 315183-21-2 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 77 mg/mL |
Water <1 mg/mL |
Ethanol 16 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02355535 | Breast Cancer|Lymphoma|Gastrointestinal Cancers|Genitourinary Cancers|Gynecologic Cancers|Head and Neck Cancers|Melanoma|Thoracic Cancers|Solid Tumors|Lymphomas | Drug: PAC-1 | Vanquish Oncology, Inc.|University of Illinois at Chicago | Phase 1 | 2015-02-01 | 2016-05-01 |
NCT02355756 | Healthy Volunteers | Drug: Maxadilan|Drug: Placebo | Universitaire Ziekenhuizen Leuven | Early Phase 1 | 2015-01-01 | 2015-07-09 |
NCT01454778 | Peripheral Vascular Disease | Drug: Paclitaxel | Patrick Kelly|Sanford Health | 2011-04-01 | 2016-04-15 | |
NCT02530762 | Signs and Symptoms, Digestive | Other: Novel Fiber|Other: Positive Fiber control|Other: Negative Control | Cargill | 2014-09-01 | 2015-08-20 | |
NCT00944996 | Major Depression | Drug: SSRI; SNRI; TCA | Tirat Carmel Mental Health Center|University of Michigan|Ariel University|The Nazareth Hospital, Israel | 2009-06-01 | 2012-07-25 | |
NCT02532985 | Signs and Symptoms, Digestive | Other: Negative Control|Other: Positive Fiber Control|Other: Novel Fiber|Other: Novel Fiber|Other: Novel Fiber | Cargill | 2014-10-01 | 2015-08-24 | |
NCT02100462 | Hypertension | Drug: Chlorthalidone 12.5 mg|Drug: Hydrochlorothiazide 25 mg|Drug: Aspirin 81 mg | Creighton University|Dialysis Clinic, Inc. | Phase 4 | 2014-03-01 | 2015-12-10 |
NCT01865136 | Pregnancy | Other: Medical Post Abortion Care | Karolinska Institutet|Kenya Medical Research Institute|University of Nairobi | Phase 4 | 2013-09-01 | 2016-08-30 |
NCT00106587 | Coronary Restenosis | Device: paclitaxel coated balloon catheter (device with drug) | University Hospital, Saarland | Phase 1|Phase 2 | 2003-12-01 | 2005-11-09 |
NCT00075686 | Pancreatic Cancer | Biological: cetuximab|Drug: gemcitabine hydrochloride | Southwest Oncology Group|National Cancer Institute (NCI)|Cancer and Leukemia Group B|NCIC Clinical Trials Group | Phase 3 | 2004-01-01 | 2015-11-16 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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