General description
一种选择性的JAK2抑制剂,IC50:3nM。
Fedratinib is a JAK2 inhibitor, is also an orally bioavailable, small-molecule, ATP-competitive inhibitor of Janus-associated kinase 2 (JAK2) with potential antineoplastic activity. JAK2 inhibitor TG101348 competes with JAK2 as well as the mutated form AK2V617F for ATP binding, which may result in inhibition of JAK2 activation, inhibition of the JAK-STAT signaling pathway, and the induction of tumor cell apoptosis. JAK2 is the most common mutated gene in bcr-abl-negative myeloproliferative disorders (MPDs); the mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival。
Fedratinib是JAK2抑制剂，也是具有潜在抗肿瘤活性的Janus相关激酶2（JAK2）的口服生物利用型，小分子，ATP竞争性抑制剂。 JAK2抑制剂TG101348与JAK2以及突变形式AK2V617F竞争ATP结合，这可能导致抑制JAK2活化，抑制JAK-STAT信号通路和诱导肿瘤细胞凋亡。 JAK2是bcr-abl阴性骨髓增生性疾病（MPD）中最常见的突变基因。 JAK2V617F的突变形式在617位具有缬氨酸到苯丙氨酸的修饰，在肿瘤细胞的增殖和存活中起着关键作用。
Properties
| Iupac Name： | N-(tert-butyl)-3-[(5-methyl-2-{4-[2-(1-pyrrolidinyl)ethoxy]anilino}-4-pyrimidinyl)amino]benzenesulfonamide |
| Inchi Code | 1S/C27H36N6O3S/c1-20-19-28-26(30-21-10-12-23(13-11-21)36-17-16-33-14-5-6-15-33)31-25(20)29-22-8-7-9-24(18-22)37(34,35)32-27(2,3)4/h7-13,18-19,32H,5-6,14-17H2,1-4H3,(H2,28,29,30,31) |
| Inchi Key | JOOXLOJCABQBSG-UHFFFAOYSA-N |
安全信息
RIDADR NONH for all modes of transport
