Pacritinib hydrochloride

Names

[ CAS No. ]:
1228923-43-0

[ Name ]:
Pacritinib hydrochloride

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> JAK
Signaling Pathways >> Epigenetics >> JAK
Signaling Pathways >> Stem Cell/Wnt >> JAK

[Target]

JAK2V617F:19 nM (IC50)

JAK3:520 nM (IC50)

JAK1:1280 nM (IC50)

JAK2wt:23 nM (IC50)

Tyk2:50 nM (IC50)


[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H32N4O3.xClH

Related Compounds

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