Pacritinib (hydrochloride)

Pacritinib hydrochloride is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM) . Pacritinib hydrochloride also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM) . Pacritinib hydrochloride can be used for the research of acute myeloid leukemia (AML) and myelofibrosis (MF) [1][2][3].

Product Specifications

CAS Number

[1228923-43-0]

Product Name Alternative

SB1518 (hydrochloride)

UNSPSC

12352211

Target

FLT3; JAK

Type

Reference compound

Related Pathways

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/SB-1518__hydrochloride__1:x_.html

Solubility

10 mM in DMSO

Smiles

[H]Cl.C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1.[x]

Molecular Formula

C28H32N4O3.xClH

References & Citations

[1]Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011 Nov;25 (11) :1751-9.|[2]Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011 Nov;1 (11) :e44.|[3]Komrokji RS, et al. Results of a phase 2 study of pacritinib (SB1518), a JAK2/JAK2 (V617F) inhibitor, in patients with myelofibrosis. Blood. 2015 Apr 23;125 (17) :2649-55.