Pacritinib

Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM) . Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM) .

Product Specifications

CAS Number

[937272-79-2]

Product Name Alternative

SB1518

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

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/pacritinib.html

Purity

99.93

Solubility

0.1 M HCl : 2 mg/mL (ultrasonic) |1 M HCl : ≥ 100 mg/mL|DMSO : 10 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

C1(COC/C=C/COCC2=C(OCCN3CCCC3)C=CC4=C2)=CC=CC(C5=N/C(NC=C5)=N\4)=C1

Molecular Formula

C28H32N4O3

Molecular Weight

472.58

Precautions

H302, H315, H319, H335

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]William AD, et al. Discovery of the macrocycle 11- (2-pyrrolidin-1-yl-ethoxy) -14,19-dioxa-5,7,26-triaza-tetracyclo[19.3.1.1 (2,6) .1 (8,12) ]heptacosa-1 (25),2 (26),3,5,8,10,12 (27),16,21,23-decaene (SB1518), a potent Janus kinase 2/fms-like tyrosine kinase-3 (JA