Potent inhibitor of JAK2
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LY2784544

Item No. 16705

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(4-chloro-2-fluorophenyl)methyl]-2-methyl-N-(5-methyl-1H-pyrazol-3-yl)-8-(4-morpholinylmethyl)-imidazo[1,2-b]pyridazin-6-amine
CAS Number
1229236-86-5
Molecular Formula
C23H25ClFN7O
Formula Weight
470.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 10 mg/ml
λmax
225, 255, 345 nm
SMILES
CC1=CC(NC2=NN3C(C(CN4CCOCC4)=C2)=NC(C)=C3CC5=C(F)C=C(Cl)C=C5)=NN1
InChi Code
InChI=1S/C23H25ClFN7O/c1-14-9-21(29-28-14)27-22-11-17(13-31-5-7-33-8-6-31)23-26-15(2)20(32(23)30-22)10-16-3-4-18(24)12-19(16)25/h3-4,9,11-12H,5-8,10,13H2,1-2H3,(H2,27,28,29,30)
InChi Key
SQSZANZGUXWJEA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $149

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    10 mg

    $263

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    25 mg

    $575

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    Product Description

    LY2784544 is a potent, ATP-competitive inhibitor of janus kinase 2 (JAK2) that less effectively inhibits JAK3 (IC50s = 3 and 48 nM, respectively).1 It also inhibits JAK2 containing the V617F mutation (IC50 = 20 nM), blocking STAT5 phosphorylation and proliferation of Ba/F3 pro-B-cells expressing this constitutively active JAK2 mutant form.1 When given by oral gavage, LY2784544 significantly reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors, reticulocytes, or platelets.1 JAK inhibitors, including LY2784544, may be useful in hematological malignancies.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ma, L., Clayton, J.R., Walgren, R.A., et al. Discovery and characterization of LY2784544, a small-molecule tyrosine kinase inhibitor of JAK2V617F. Blood Cancer J. 3(4), e109 (2013).

    2. Furqan, M., Mukhi, N., Lee, B., et al. Dysregulation of JAK-STAT pathway in hematological malignancies and JAK inhibitors for clinical application. Biomark. Res. 1(1), 5 (2013).