An equipotent inhibitor of FLT3 and JAK2
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Pacritinib

Item No. 16709

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
11-[2-(1-pyrrolidinyl)ethoxy]-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),16E,21,23-decaene
CAS Number
937272-79-2
Synonyms
  • SB1518
Molecular Formula
C28H32N4O3
Formula Weight
472.6
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: .5 mg/ml (slightly warmed)
λmax
285 nm
SMILES
C12=C(OCCN3CCCC3)C=CC(/N=C4N=CC=C(C5=CC=CC(COC/C=C/COC2)=C5)N/4)=C1
InChi Code
InChI=1S/C28H32N4O3/c1-2-13-32(12-1)14-17-35-27-9-8-25-19-24(27)21-34-16-4-3-15-33-20-22-6-5-7-23(18-22)26-10-11-29-28(30-25)31-26/h3-11,18-19H,1-2,12-17,20-21H2,(H,29,30,31)/b4-3+
InChi Key
HWXVIOGONBBTBY-ONEGZZNKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $49

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    1 mg

    $93

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    5 mg

    $376

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    Product Description

    Pacritinib is an inhibitor of both FLT3 and JAK2 (IC50s = 22 and 23 nM, respectively).1 It also blocks the activities of the FLT3 D835Y mutant, FLT3 with internal tandem duplications (ITDs), and JAK2 with a V617F substitution (IC50s = 6, 20-180, and 220 nM, respectively).1 Pacritinib also inhibits JAK1, JAK3, and TYK2 (IC50s = 1280, 520, and 50 nM, respectively).1 Pacritinib is orally bioavailable, inhibiting FLT3 and JAK2 signaling, tumor growth, and metastasis in xenografts in mice.1 It is synergistic with the histone deacetylase inhibitor pracinostat (also known as SB 939, Item No. 10443), decreasing cell proliferation and inducing apoptosis in cells carrying either the JAK2 V617F mutation or FLT3 with ITDs, both in vitro and in vivo.2 Pacritinib has potential in resolving hematological malignancies.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hart, S., Goh, K.C., Novotny-Diermayr, V., et al. Pacritinib (SB1518), a JAK2/FLT3 inhibitor for the treatment of acute myeloid leukemia. Blood Cancer J. 1(11), 1-9 (2011).

    2. Novotny-Diermayr, V., Hart, S., Goh, K.C., et al. The oral HDAC inhibitor pracinostat (SB939) is efficacious and synergistic with the JAK2 inhibitor pacritinib (SB1518) in preclinical models of AML. Blood Cancer J. 2(5), 1-10 (2012).

    3. Hatzimichael, E., Tsolas, E., and Briasoulis, E. Profile of pacritinib and its potential in the treatment of hematologic disorders. J. Blood Med. 5, 143-152 (2014).