CHZ868,a type II JAK inhibitor, would demonstrate activity in JAK inhibitor persistent cells, murine MPN models, and MPN patient samples. JAK2 and MPL mutant cell lines were sensitive to CHZ868, including type I JAK inhibitor persistent cells. CHZ868 showed significant activity in murine MPN models and induced reductions in mutant allele burden not observed with type I JAK inhibitors. These data demonstrate that type II JAK inhibition is a viable therapeutic approach for MPN patients.
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化学信息
名称 | CHZ868(CHZ-868) |
Iupac 化学名称 | N-(4-((2-((2,4-difluorophenyl)amino)-1,4-dimethyl-1H-benzo[d]imidazol-5-yl)oxy)pyridin-2-yl)acetamide |
同义词 | CHZ 868;CHZ-868;CHZ868 |
英文同义词 | CHZ 868;CHZ-868;CHZ868 |
分子式 | C22H19F2N5O2 |
分子量 | 423.42 |
Smile | CN1C2=CC=C(OC3=CC=NC(NC(C)=O)=C3)C(C)=C2N=C1NC4=CC=C(F)C=C4F |
InChiKey | KQQLBXFPTDVFAJ-UHFFFAOYSA-N |
InChi | InChI=1S/C22H19F2N5O2/c1-12-19(31-15-8-9-25-20(11-15)26-13(2)30)7-6-18-21(12)28-22(29(18)3)27-17-5-4-14(23)10-16(17)24/h4-11H,1-3H3,(H,27,28)(H,25,26,30) |
Cas号 | 1895895-38-1 |
相关CAS号 | |
外观性状 | crystalline solid |
纯度 | 98% by HPLC |
存储 | 3 years -20ºCpowder 6 months-80ºCin solvent |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |