产品说明书
Tipifarnib
 |
同义名 : | 提法法尼 ;R115777;IND 58359;trade name Zarnestra;D03720;NSC702818;LX81 |
| CAS号 : | 192185-72-1 | |
| 货号 : | A412936 | |
| 分子式 : | C27H22Cl2N4O | |
| 纯度 : | 99%+ | |
| 分子量 : | 489.396 | |
| MDL号 : | MFCD07772347 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 105 mg/mL(214.55 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 |
|
| 动物实验配方： |
IP 2% DMSO+water 0.5 mg/mL clear PO 0.5% CMC-Na 18 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
|
||
| 描述 | Farnesylation is a posttranslational modification of proteins by which an isoprenyl group is added to a cysteine residue. In mammalian cells, newly synthesized proteins like Ras must be posttranslationally modified by farnesylation through farnesyl protein transferase to allow its proper membrane localization. Tipifarnib is a potent and selective farnesyl protein transferase (FPT) inhibitor with IC50 values of 0.86 nM and 7.9 nM for inhibition of the farnesylation of lamin B and K-RasB peptide substrates, respectively. Treatment with Tipifarnib at concentration ranging in 5-50nM for 3 days inhibited Ras (p21ras) processing in intact NIH 3T3 cells stably transfected with the T24 H-ras oncogene cells, observed by ratio of soluble and total particulate fractions. Tipifarnib exhibited a panel of human tumor cell lines of various tissue types with wide-type ras gene with IC50 values ranging in 2.7-111nM. Oral administration of Tipifarnib at dose ranging in 6.25–100 mg/kg, b.i.d, dose-dependently inhibited the growth of tumors bearing mutant H-ras, mutant K-ras, and wild-type ras genes in nude mice bearing s.c. tumors. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| human 786-0 cell | Growth inhibition assay | Inhibition of human 786-0 cell growth in a cell viability assay, IC50=0.32173 μM | SANGER | ||
| human 8505C cell | Growth inhibition assay | Inhibition of human 8505C cell growth in a cell viability assay, IC50=0.43109 μM | SANGER | ||
| human A375 cell | Growth inhibition assay | Inhibition of human A375 cell growth in a cell viability assay, IC50=0.61648 μM | SANGER | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00076102 | Neurofibromatosis 1 ... 展开 >> Neurofibroma, Plexiform 收起 << | Phase 2 | Completed | - | United States, Alabama ... 展开 >> University of Alabama Birmingham, Alabama, United States, 35233 United States, District of Columbia Childrens National Medical Center Washington, District of Columbia, United States, 20010 United States, Illinois Childrens Memorial Hospital, Chicago Chicago, Illinois, United States, 60614 United States, Maryland Johns Hopkins Oncology Center Baltimore, Maryland, United States, 21287 National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 United States, Massachusetts Childrens Hospital, Dana-Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic, Rochester Rochester, Minnesota, United States, 55905 United States, Missouri St. Louis Children's Hospital Saint Louis, Missouri, United States, 63110 United States, New York Beth Israel Medical Center New York, New York, United States, 10003 SUNY Upstate Medical University Syracuse, New York, United States, 13210 United States, Ohio Cleveland Clinic Cleveland, Ohio, United States, 44195 United States, Oregon Oregon Health Sciences University Portland, Oregon, United States, 97201-3098 United States, Pennsylvania Childrens Hospital, Philadelphia Philadelphia, Pennsylvania, United States, 19104 Childrens Hospital, Pittsburgh Pittsburgh, Pennsylvania, United States, 15213 United States, Texas Texas Children's Hospital Houston, Texas, United States, 77030 收起 << |
| NCT00076102 | - | Completed | - | - | |
| NCT02845232 | - | Completed | - | France ... 展开 >> Hospices Civils de Lyon - Centre Hospitalier Lyon Sud, 165 Chemin du Grand Revoyet Pierre-benite, France, 69310 收起 << | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.04mL 0.41mL 0.20mL |
10.22mL 2.04mL 1.02mL |
20.43mL 4.09mL 2.04mL |
