磷酸蘆可替尼是一種有效的 JAK1/2 抑制劑， IC50 分別為3.3 nM/2.8 nM，比JAK3選擇性高130倍。

Ruxolitinib（INCB018424）有效且選擇性地抑制JAK2V617F介導(dǎo)的信號傳導(dǎo)和增殖。 Ruxolitinib抑制HEL細胞的生長，EC50為186 nM。 Ruxolitinib顯著增加Ba / F3-EpoR-JAK2V617F細胞系統(tǒng)的凋亡，并抑制原發(fā)性MPN患者樣本中的造血祖細胞增殖。Ruxolitinib（180 mg / kg，po）可降低接種JAK2V617F表達細胞的小鼠的腫瘤負荷，而不會引起貧血或淋巴細胞減少。

磷酸蘆可替尼 (INCB018424, INC424)是蘆可替尼的磷酸鹽形式。蘆可替尼是第一個應(yīng)用于臨床的，有效的，選擇性JAK1/2抑制劑，在無細胞試驗中IC50為3.3 nM/2.8 nM。作用于JAK1，JAK2與作用于JAK3相比，選擇性高130多倍。蘆可替尼通過毒性線粒體自噬殺死腫瘤細胞。蘆可替尼可誘導(dǎo)自噬并增強細胞凋亡。

Target	Value
JAK2 (Cell-free assay)	2.8 nM
JAK1 (Cell-free assay)	3.3 nM

一種有效的JAK1/2抑制劑,IC50 分別為3.3 nM/2.8 nM，比JAK3選擇性高130倍。
Ruxolitinib is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.