P1 41 was a Skp2 inhibitor and was thought to prevent assembly of Skp2-Skp1 complexes.
Selectively suppresses Skp2 SCF E3 ligase activity but exhibits no effect on the activity of other SCF complexes. Also inhibits Skp2-mediated p27 and Akt ubiquitination in vivo and in vitro. Suppresses the survival of cancer cells and cancer stem cells by triggering cell senescence and inhibiting glycolysis. Exhibits antitumor effects in multiple animal models and cancer cell lines.
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] Chan et al (2013) Pharmacological inactivation of Skp2 SCF ubiquitin ligase restricts cancer stem cell traits and cancer progression. Cell 154 556. PMID:23911321 .
分子式 C24H24N2O3S |
分子量 420.52 |
CAS号 222716-34-9 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 5 mM warmed |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00866307 | B-cell Adult Acute Lymphoblastic Leukemia|B-cell Childhood Acute Lymphoblastic Leukemia|Untreated Adult Acute Lymphoblastic Leukemia|Untreated Childhood Acute Lymphoblastic Leukemia | Drug: pegaspargase|Drug: cytarabine|Drug: vincristine sulfate|Drug: doxorubicin hydrochloride|Drug: cyclophosphamide|Drug: prednisone|Drug: dexamethasone|Drug: methotrexate|Drug: daunorubicin hydrochloride|Drug: mercaptopurine|Drug: thioguanine|Radiation: prophylactic cranial irradiation|Other: laboratory biomarker analysis | Children's Oncology Group|National Cancer Institute (NCI) | 2009-02-01 | 2017-02-07 | |
NCT02237664 | Video-assisted Thoracoscopic Surgery | Procedure: Continuous paravertebral analgesia (C-PVB)|Procedure: Patient-controlled paravertebral analgesia (PC-PVB) | Dammam University | Phase 1|Phase 2 | 2015-01-01 | 2015-04-03 |
NCT02612103 | Inflammatory Bowel Disease|Colitis, Ulcerative|Crohn Disease | Line Elberg Godskesen|University of Southern Denmark|Odense University Hospital | 2015-11-01 | 2016-10-11 | ||
NCT03086707 | Smokers|Never Smokers | Other: Cigarette | Philip Morris Products S.A. | 2017-01-21 | 2017-03-21 | |
NCT03020667 | Smoking|Tobacco Product | Philip Morris Products S.A. | 2016-04-01 | 2017-01-11 | ||
NCT01055314 | Adult Rhabdomyosarcoma|Childhood Alveolar Rhabdomyosarcoma|Childhood Embryonal Rhabdomyosarcoma|Metastatic Childhood Soft Tissue Sarcoma|Stage IV Adult Soft Tissue Sarcoma|Untreated Childhood Rhabdomyosarcoma | Biological: Cixutumumab|Drug: Cyclophosphamide|Biological: Dactinomycin|Drug: Doxorubicin Hydrochloride|Drug: Etoposide|Drug: Ifosfamide|Drug: Irinotecan Hydrochloride|Other: Laboratory Biomarker Analysis|Drug: Temozolomide|Drug: Vincristine Sulfate Liposome | National Cancer Institute (NCI) | Phase 2 | 2010-01-01 | 2015-05-22 |
NCT01197300 | Osteoporosis | Drug: zoledronic acid | Novartis Pharmaceuticals|Novartis | Phase 3 | 2010-10-01 | 2016-06-10 |
NCT00404820 | Osteoporosis | Drug: Zoledronic acid 5 mg solution|Drug: Alendronate 70 mg tablets|Drug: Calcium/Vitamin D | Novartis | Phase 3 | 2006-10-01 | 2011-06-06 |
NCT02445365 | Colitis, Ulcerative|Gastrointestinal Diseases|Pathologic Processes|Intestinal Diseases|Inflammatory Bowel Diseases | Device: AutoRIC device | Odense University Hospital|University of Southern Denmark|Aarhus University Hospital | 2015-05-01 | 2016-10-11 | |
NCT02681315 | Prematurity, Mechanical Ventilation | Device: HHHFNC 6 liter minute|Device: HHHFNC 3 liters/min | Mansoura University Children Hospital | Phase 3 | 2016-03-01 | 2016-09-16 |
NCT02510911 | Postoperative Ileus|Laparoscopic Colectomy Without Stoma Formation|Colorectal Neoplasm|Diverticulitis | Drug: Caffeine (100 mg)|Drug: Caffeine (200 mg)|Drug: corn starch (250 mg approx.)|Other: Radiopaque marker | Thomas Steffen|Gottfried und Julia Bangerter-Rhyner Foundation, Switzerland|Cantonal Hospital of St. Gallen | 2015-08-01 | 2016-04-06 |
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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