A potent inhibitor of Pim kinases
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SGI-1776

Item No. 16423

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine
CAS Number
1025065-69-3
Synonyms
  • Pim-Kinase Inhibitor IX
Molecular Formula
C20H22F3N5O
Formula Weight
405.4
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 10 mg/mlEthanol: 30 mg/ml
λmax
212, 271, 343 nm
SMILES
CN1CCC(CNC(C=C2)=NN3C2=NC=C3C4=CC=CC(OC(F)(F)F)=C4)CC1
InChi Code
InChI=1S/C20H22F3N5O/c1-27-9-7-14(8-10-27)12-24-18-5-6-19-25-13-17(28(19)26-18)15-3-2-4-16(11-15)29-20(21,22)23/h2-6,11,13-14H,7-10,12H2,1H3,(H,24,26)
InChi Key
MHXGEROHKGDZGO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $236

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    50 mg

    $835

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    Product Description

    The Pim family proteins are serine/threonine kinases involved in cancer progression.1 SGI-1776 is a potent inhibitor of all three human Pim kinases (IC50s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively).2 While it also inhibits FLT3 and haspin (IC50s = 44 and 34 nM, respectively), SGI-1776 has little effect on several other kinases, including cell cycle kinases.2 SGI-1776 induces apoptosis in lymphocytes from patients with chronic or acute lymphocytic leukemia but not in those from healthy donors.2,3 At 10 µM, it reduces STAT3 phosphorylation without reducing STAT3 expression in cancer cells, and this correlates with inhibition of cell proliferation.4 SGI-1776 also enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant prostate cancer cells to taxanes.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Beharry, Z., Mahajan, S., Zemskova, M., et al. The Pim protein kinases regulate energy metabolism and cell growth. Proc. Natl. Acad. Sci. USA 108(2), 528-533 (2011).

    2. Chen, L.S., Redkar, S., Bearass, D., et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells. Blood 114(19), 4150-4157 (2009).

    3. Chen, L.S., Redkar, S., Taverna, P., et al. Mechanisms of cytotoxicity to Pim kinase inhibitor, SGI-1776, in acute myeloid leukemia. Blood 118(3), 693-702 (2011).

    4. Chang, M., Kanwar, N., Feng, E., et al. PIM kinase inhibitors downregulate STAT3Tyr705 phosphorylation. Mol. Cancer Ther. 9(9), 2478-2487 (2010).

    5. Mahalingam, D., Espitia, C.M., Medina, E.C., et al. Targeting PIM kinase enhances the activity of sunitinib in renal cell carcinoma. Br. J. Cancer 105(10), 1563-1573 (2011).

    6. Mumenthaler, S.M., Ng, P.Y.B., Hodge, A., et al. Pharmacologic inhibition of Pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. Mol. Cancer Ther. 8(10), 2882-2893 (2009).