Pacritinib Inhibitor CAS No. 937272-79-2

Cat. No.	Name	Size	Price	Add Cart
KI1293	Pacritinib	5 mg	$480

Chemical Characteristic

Product Name	Pacritinib
Synonyms	SB1518
CAS No.	937272-79-2
Molecular Weight	472.58
Formula	C₂₈H₃₂N₄O₃
Chemical Name	14,19-Dioxa-5,7,27-triazatetracyclo[19.3.1.12,6.18,12]heptacosa-1(25),2,4,6(27),8,10,12(26),16,21,23-decaene, 11-[2-(1-pyrrolidinyl)ethoxy]-, (16E)-
Smiles	c12c3ccnc(Nc4ccc(c(COC/C=C/COCc(ccc1)c2)c4)OCCN1CCCC1)n3
Chemical Structure

Biological activities

Pacritinib is a novel oral JAK2 inhibitor. Pacritinib inhibits JAK2^WT and JAK2^V617F with IC50 of 23 and 19 nM, respectively. Pacritinib also inhibits JAK1, JK3, TYK2 and fms-like tyrosine kinase-3 (FLT3) with IC50 of 1280, 520, 50 and 22 nM, respectively. Pacritinib has potent anti-proliferative effects on myeloid and lymphoid cell lines driven by mutant or wild-type JAK2 or FLT3, resulting from cell cycle arrest and induction of apoptosis. Pacritinib significantly reduces splenomegaly and hepatomegaly in a JAK2^V617F-driven disease model. Pacritinib dose-dependently inhibits intra-tumor JAK2/STAT5 signaling, leading to tumor growth inhibition in a subcutaneous model generated with SET-2 cells.^[1] Pacritinib inhibits FLT3 phosphorylation and downstream STAT, MAPK and PI3?K signaling in FLT3-internal-tandem duplication (ITD), FLT3-wt cells and primary AML blast cells. Oral administration of pacritinib in murine models of FLT3-ITD-driven AML leads to significant inhibition of primary tumor growth and lung metastasis. ^[2]

Protocols

Pacritinib is dissolved in DMSO. ^[1]

References

[1] Hart S, et al. SB1518, a novel macrocyclic pyrimidine-based JAK2 inhibitor for the treatment of myeloid and lymphoid malignancies. Leukemia. 2011, 25 (11): 1751-1759. [2] Hart S, et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 2011, 1 (11): e44

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