产品说明书
Momelotinib
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同义名 : | CYT387;LM-1149 ;CYT11387 |
| CAS号 : | 1056634-68-4 | |
| 货号 : | A207449 | |
| 分子式 : | C23H22N6O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 414.46 | |
| MDL号 : | MFCD16038899 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,2-8°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 9 mg/mL(21.72 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 |
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| 动物实验配方： |
IP 2% DMSO+2% Tween80+40% PEG300+water 6 mg/mL clear PO 0.5% CMC-Na 35 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | CYT387 (Momelotinib) is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 11 nM and 18 nM while less activity against other kinases including JAK3 (IC50 = 155 nM). MECNISIM. CYT387 inhibits proliferation of JAK2V617F mutation HEL cells as well as Ba/F3-wt and Ba/F3-JAK2V67F cells with IC50 of approximately 1400~1500 nM. Proliferation of Ba/F3-MPLW515L cell was also inhibited with IC50 = 200 nM. In human erythroleukemia (HEL) cells, CYT387 inhibits phosphorylation of STAT-5 and STAT-3 with IC50s of 400 nM and 2500 nM. Besides, CYT387 can also inhibit in vitro erythroid colony formation in polycythemia vera patients.[1]Together with paclitaxel, CYT387-treated human ovarian HEY cells showed a significant reduced tumor burden compared to that with paclitaxel only-treated transplanted cells in mice.[2] CYT387 could be used in the treatment of primary myelofibrosis or post-polycythemia vera or post-essential thrombocythemia myelofibrosis (post-PV/ET MF), as well as the treatment for relapsed or refractory metastatic pancreatic ductal adenocarcinoma (in combination with capecitabine and oxaliplatin). | ||
| 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 HEL 92.1.7 cells | Proliferation assay | 72 h | Antiproliferative activity against human HEL 92.1.7 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=1.804 μM | 19762238 | |
| human SET2 cells | Proliferation assay | 72 h | Antiproliferative activity against human SET2 cells expressing JAK2 V617F mutant kinase after 72 hrs by alamar blue assay, IC50=0.232 μM | 19762238 | |
| mouse BAF3 cells | Proliferation assay | 72 h | Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay | 19762238 | |
| 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 |
| NCT02251821 | Primary Myelofibrosis ... 展开 >> Secondary Myelofibrosis 收起 << | Phase 2 | Recruiting | - | United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Rachel B. Salit 206-667-1317 rsalit@fredhutch.org Principal Investigator: Rachel B. Salit 收起 << |
| NCT02206763 | EGFR Mutated EGFR TKI Naive Me... 展开 >>tastatic NSCLC 收起 << | Phase 1 | Terminated | - | United States, California ... 展开 >> Duarte, California, United States Palo Alto, California, United States Whittier, California, United States 收起 << |
| NCT01998828 | Polycythemia Vera ... 展开 >> Essential Thrombocythemia 收起 << | Phase 2 | Terminated | - | United States, Arizona ... 展开 >> Scottsdale, Arizona, United States United States, California Whittier, California, United States United States, Mississippi Tupelo, Mississippi, United States United States, Missouri Saint Louis, Missouri, United States United States, Texas Houston, Texas, United States Australia, Victoria Frankston, Victoria, Australia Parkville, Victoria, Australia Canada, Ontario Toronto, Ontario, Canada Canada, Quebec Montreal, Quebec, Canada Canada Vancouver, Canada France La Tronche, France Nantes Cedex 1, France Paris, France Germany Dresden, Germany Minden, Germany 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.06mL 2.41mL 1.21mL |
24.13mL 4.83mL 2.41mL |
