CYT387是一种ATP竞争性JAK1/JAK2抑制剂,IC50为11 nM/18 nM,比作用于JAK3选择性约高10倍左右。
CYT387 is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively.
30% PEG400+0.5% Tween80+5% propylene glycol
0 -10 μM
≤50 mg/kg 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] Pardanani A, et al. Leukemia, 2009, 23(8), 1441-1445.
分子式 C23H22N6O2 |
分子量 414.46 |
CAS号 1056634-68-4 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 75 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT02124746 | Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis|Polycythemia Vera|Essential Thrombocythemia | Drug: Momelotinib | Gilead Sciences | Phase 2 | 2014-04-01 | 2017-02-28 |
NCT01998828 | Polycythemia Vera|Essential Thrombocythemia | Drug: Momelotinib | Gilead Sciences | Phase 2 | 2014-02-01 | 2016-04-26 |
NCT02101268 | Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV)|Post-essential Thrombocythemia Myelofibrosis (Post-ET MF) | Drug: Momelotinib|Drug: Best Available Therapy (BAT) | Gilead Sciences | Phase 3 | 2014-06-01 | 2017-02-13 |
NCT01969838 | Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis | Drug: Momelotinib|Drug: Ruxolitinib|Drug: Placebo to match momelotinib|Drug: Placebo to match ruxolitinib | Gilead Sciences | Phase 3 | 2013-12-01 | 2017-01-05 |
NCT02101021 | Metastatic Pancreatic Ductal Adenocarcinoma | Drug: Momelotinib|Drug: Placebo to match momelotinib|Drug: Nab-paclitaxel|Drug: Gemcitabine | Gilead Sciences | Phase 3 | 2014-06-02 | 2017-03-21 |
NCT01423058 | Primary Myelofibrosis|Post-Polycythemia Vera|Post-Essential Thrombocythemia Myelofibrosis | Drug: Momelotinib | Gilead Sciences | Phase 1|Phase 2 | 2011-08-01 | 2015-01-16 |
NCT02515630 | Primary Myelofibrosis (PMF)|Post-polycythemia Vera (Post-PV) Myelofibrosis|Postessential Thrombocythemia (Post-ET) Myelofibrosis | Drug: MMB | Gilead Sciences | Phase 2 | 2016-01-29 | 2017-02-16 |
NCT02244489 | Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma | Drug: MMB|Drug: Capecitabine|Drug: Oxaliplatin | Gilead Sciences | Phase 1 | 2014-11-01 | 2016-12-21 |
NCT02258607 | Relapsed Metastatic KRAS-Mutated Non-Small Cell Lung Cancer | Drug: MMB|Drug: Trametinib | Gilead Sciences | Phase 1 | 2015-03-01 | 2016-08-04 |
NCT02206763 | EGFR Mutated EGFR TKI Naive Metastatic NSCLC | Drug: MMB|Drug: Erlotinib | Gilead Sciences | Phase 1 | 2014-10-16 | 2017-03-20 |
NCT01236638 | Primary Myelofibrosis|Post-Polycythemia Vera Myelofibrosis|Post-Essential Thrombocythemia Myelofibrosis | Drug: Momelotinib | Gilead Sciences | Phase 2 | 2010-11-01 | 2014-07-11 |
NCT02251821 | Primary Myelofibrosis|Secondary Myelofibrosis | Procedure: Allogeneic Hematopoietic Stem Cell Transplantation|Drug: Busulfan|Drug: Cyclophosphamide|Drug: Fludarabine Phosphate|Other: Laboratory Biomarker Analysis|Drug: Melphalan|Drug: Methotrexate|Drug: Momelotinib|Drug: Mycophenolate Mofetil|Drug: Pacritinib|Drug: Ruxolitinib|Drug: Tacrolimus|Radiation: Total-Body Irradiation|Procedure: Umbilical Cord Blood Transplantation | Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI)|National Heart, Lung, and Blood Institute (NHLBI) | Phase 2 | 2014-10-01 | 2016-11-29 |
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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