Ruxolitinib phosphate 是一种JAK1/2抑制剂，IC50分别为3.3 nM/2.8 nM，对 JAK1/2 的选择性是 JAK3 的 130 倍以上。

Ruxolitinib phosphate(INCB018424 phosphate) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.

Ruxolitinib (INCB018424) potently and selectively inhibits JAK2V617F-mediated signaling and proliferation. Ruxolitinib inhibits the growth of HEL cells with EC50 of 186 nM. Ruxolitinib markedly increases apoptosis in Ba/F3-EpoR-JAK2V617F cell system. It also inhibits hematopoietic progenitor cell proliferation in primary MPN patient samples[1].

Ruxolitinib (180 mg/kg, p.o.) reduces the tumor burden of mice inoculated with JAK2V617F-expressing cells while not causing anemia or lymphopenia[1].

Ruxolitinib phosphate is dissolved in 0.2% DMSO. Cells are seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability is measured by cellular ATP determination using the Cell-Titer Glo luciferase reagent or viable cell counting. Values are transformed to percent inhibition relative to vehicle control, and IC50?curves are fitted according to nonlinear regression analysis of the data using PRISM GraphPad.

1092939-17-7

C17H21N6O4P

404.367

INC424;INCB018424;INC 424 phosphate;INCB018424 phosphate;磷酸鲁索利替尼;Ruxolitinib (INCB-18424) phosphate

H2O:8 mg/mL(19.8 mM)
DMSO:70 mg/mL(173.1 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years