XL019

XL019 is a potent, orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2[1][2].

Product Specifications

CAS Number

[945755-56-6]

UNSPSC

12352005

Hazard Statement

H372

Target

Apoptosis; JAK

Type

Reference compound

Related Pathways

Apoptosis; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/xl019.html

Purity

99.65

Solubility

DMSO : 25 mg/mL (ultrasonic)

Smiles

O=C([C@H]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2

Molecular Formula

C25H28N6O2

Molecular Weight

444.53

Precautions

H372

References & Citations

[1]Forsyth T, et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22 (24) :7653-8.