SGI-<wbr/>1776

SGI-1776

CAT N°: 16423
Price:

From 48.00 40.80

The Pim family proteins are serine/threonine kinases involved in cancer progression.{20750} 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).{26823} 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.{26823} SGI-1776 induces apoptosis in lymphocytes from patients with chronic or acute lymphocytic leukemia but not in those from healthy donors.{26823,26824} At 10 µM, it reduces STAT3 phosphorylation without reducing STAT3 expression in cancer cells, and this correlates with inhibition of cell proliferation.{26826} SGI-1776 also enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant prostate cancer cells to taxanes.{26827,26825}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine
  • Correlated keywords
    • inhibitors cancers apoptosis proteins kinases intracellular signaling Pims SGI1776 SGIs 1776 potent humans Flt-3 Flts 3 Flt3 haspin cells cycles induces inductions inducing lymphocytes patients chronic acute lymphocytic leukemia healthy donors reduces reductions reduced reducing STAT3 STATs STAT-3 phosphorylation expressions inhibitions inhibits proliferations sunitinib activity activities renal carcinomas resensitizes chemoresistant chemoresistance resistant resistance prostates taxanes biochemicals IX P
  • Product Overview:
    The Pim family proteins are serine/threonine kinases involved in cancer progression.{20750} 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).{26823} 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.{26823} SGI-1776 induces apoptosis in lymphocytes from patients with chronic or acute lymphocytic leukemia but not in those from healthy donors.{26823,26824} At 10 µM, it reduces STAT3 phosphorylation without reducing STAT3 expression in cancer cells, and this correlates with inhibition of cell proliferation.{26826} SGI-1776 also enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant prostate cancer cells to taxanes.{26827,26825}

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