A potent inhibitor of all three human Pim kinases (IC50s = 7

SGI-1776 – 1 mg

Brand:
Cayman
CAS:
1025065-69-3
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

A potent inhibitor of all three human Pim kinases (IC50s = 7, 363, and 69 nM for Pim-1, Pim-2, and Pim-3, respectively); induces apoptosis in lymphocytes from patients with CML or ALL; enhances the activity of sunitinib against renal cell carcinoma and resensitizes chemoresistant cancer cells to taxanes

Formal name: N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine

Synonyms:  Pim-Kinase Inhibitor IX

Molecular weight: 405.4

CAS: 1025065-69-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Kinase Inhibitors|PIMs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling||Research Area|Cancer|Multidrug Resistance

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