SGI-1776

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SGI-1776

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Cat No: 16423

Biochemicals - Kinase Inhibitors

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 inhibi...

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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}

Size	1 mg
Shipping	dry ice
CAS Number	1025065-69-3
Molecular Formula	C₂₀H₂₂F₃N₅O
SMILES	CN1CCC(CNC(C=C2)=NN3C2=NC=C3C4=CC=CC(OC(F)(F)F)=C4)CC1
Molecular Weight	405,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2922.19
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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