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XL019 945755-56-6

Product Description

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Molecular Weight:

444.53 XL019 is a potent and selective JAK2 inhibitor with IC50 of 2.2 nM, exhibiting >50-fold selectivity over JAK1, JAK3 and TYK2. Phase 1.


Biological Activity


XL019 is a highly selective JAK2 inhibitor, binds to the active site of
JAK2 displaying >50-fold selectivity against JAK1 and TYK2. XL019
reveals a desirable CYP (1A2, 2C9, 2D6, 3A4 ≥20 μM), hERG (16 μM), and
P-glycoprotein inhibition (>20 μM) profile. XL019
inhibits the activation of JAK2 as well as the mutated form JAK2V617F,
which may result in the inhibition of the JAK-STAT signaling pathway and
may induce Apoptosis. XL019 showed more than 10-fold selective
inhibition (IC50 = 64 nM) of STAT5 phosphorylation following EPO
stimulation of erythroid cells compared with other cell systems.


XL019 significantly inhibits downstream markers pSTAT1 and pSTAT3 after
administration 30, 100, and 300 mg/kg resulting in an ED50 of 42 mg/kg
(pSTAT1) and 210 mg/kg (pSTAT3). XL019 has a superior pharmacodynamic
profile and exhibits good oral absorption, and modest clearance and half
life across species. XL019 inhibits of HEL.92.1.7 xenograft tumors
growth in mice. It demonstrates 60% and 70% inhibition when dosed orally
at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Dosing
at 300 mg/kg bid provided an 11.3-fold increase in apoptosis relative
to vehicle control.

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Product Categories : Epigenetics > JAK Inhibitor