产品名称

鲁索利替尼(Ruxolitinib (INCB018424))

一般描述

Ruxolitinib(鲁索利替尼) is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.

别 称

(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile

纯 度

≥98.0%(HPLC)

CAS NO.

941678-49-5

分子式

C¹⁷H¹⁸N⁶

分子量

306.37

适用范围

生物试剂，适用于细胞培养等

l  理化信息

外 观

固体

溶解性(25℃)

DMSO

≥50mg/mL

乙醇

≥50mg/mL

水

Insoluble

l  生物学信息

生物活性/药理作用

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 tranion) 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.

Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

应 用

Ruxolitinib is a Janus kinase inhibitor that is used in the treatment of intermediate or high risk myelofibrosis. Ruxolitinib is associated with transient and usually mild elevations in serum aminotransferase during therapy, but has not been ed to cases of clinically apparent idiosyncratic acute liver injury but has been shown to be a cause of reactivation of hepatitis B.

l  存储

存储温度

-20℃

l  注意事项及免责声明

本产品仅用于实验研究，不得作为药物使用，不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov