PAC-1

Procaspase activating compound 1,PAC 1,PAC1

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。

目录号
EY1519
EY1519
EY1519
EY1519
纯度
99.14%
99.14%
99.14%
99.14%
规格
5 mg
10 mg
50 mg
100 mg
原价
260
486
1320
2400
售价
260
486
1320
2400
库存
现货
现货
现货
现货
订购
订购
订购
订购
订购
订购
  • 生物活性

    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.

  • 体外研究

  • 体内研究

  • 激酶实验

  • 细胞实验

    ~100 μM

  • 动物实验

    ~100 mg/kg颗粒皮下移植或口服处理

  • 不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 AKm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。


  • 参考文献

    [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

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    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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