For research use only.

Catalog No.S7036

4 publications

XL019 Chemical Structure

CAS No. 945755-56-6

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.

Selleck's XL019 has been cited by 4 publications

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Biological Activity

Description 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.
Features Orally bioavailable JAK2-selective inhibitor and has been tested in Phase I clinical trials for treatment of Myelofibrosis.
JAK2 [1]
(Cell-free assay)
PDGFRβ [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
FLT3 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
2.2 nM 125.4 nM 134.3 nM 139.7 nM 214.2 nM
In vitro

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. [1] 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. [2]

In vivo 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. [1]


Animal Research:[1]
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  • Animal Models: HEL.92.1.7 xenograft
  • Dosages: 100 mg/kg, 200 mg/kg, 300 mg/kg, bid
  • Administration: P.O.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 16 mg/mL (35.99 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 444.53


CAS No. 945755-56-6
Storage powder
in solvent
Synonyms N/A
Smiles C1CC(NC1)C(=O)NC2=CC=C(C=C2)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCOCC5

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00595829 Terminated Drug: XL019 Polycythemia Vera Exelixis December 2007 Phase 1
NCT00522574 Terminated Drug: XL019 Myeloproliferative Disorders|Myelofibrosis|Polycythemia Vera|Thrombocythemia Essential Exelixis August 2007 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID