Entospletinib (GS-9973)
- русский язык имя
- английское имяEntospletinib (GS-9973)
- CAS №1229208-44-9
- CBNumberCB92703799
- ФормулаC23H21N7O
- мольный вес411.46
- EINECS-0
- номер MDLMFCD28099806
- файл Mol1229208-44-9.mol
химическое свойство
плотность | 1.45±0.1 g/cm3(Predicted) |
температура хранения | Desiccate at -20°C |
растворимость | insoluble in EtOH; insoluble in H2O; ≥20.55 mg/mL in DMSO |
форма | solid |
пка | 12.54±0.40(Predicted) |
цвет | White to gray |
FDA UNII | 6I3O3W6O3B |
Словарь наркотиков NCI | entospletinib |
Entospletinib (GS-9973) химические свойства, назначение, производство
Описание
Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. GS-9973 is a potent Syk inhibitor (IC50 = 7.7 nM) that demonstrates 10-35-fold selectivity for Syk over a panel of 359 nonmutant kinases. In conjunction with the PI3Kδ inhibitor CAL-101 , it has been used to reduce chronic lymphocytic leukemia cell survival and to disrupt chemokine signaling at nanomolar concentrations.Использование
GS 9973 is a selective and orally bioavailable inhibitor of spleen tyrosine kinase (Syk).Entospletinib (GS-9973) поставщик
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