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| | SGI-1776 Basic information |
| Product Name: | SGI-1776 | | Synonyms: | N-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine;N-[(1-Methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine SGI-1776;SGI-1776;SGI-1776 free base;N-[(1-Methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine;SGI-1776, >=98%;SGI-1776 free base
N-[(1-Methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-imidazo[1,2-b]pyridazin-6-amine;SGI-1776 FREE BASE;SGI1776 | | CAS: | 1025065-69-3 | | MF: | C20H22F3N5O | | MW: | 405.42 | | EINECS: | 200-258-5 | | Product Categories: | Inhibitors;JAK;Inhibitor;JAK/STAT;STAT | | Mol File: | 1025065-69-3.mol |  |
| | SGI-1776 Chemical Properties |
| density | 1.37 | | storage temp. | Store at -20°C | | solubility | ≥40.5 mg/mL in DMSO; insoluble in H2O; ≥101 mg/mL in EtOH | | pka | 9.22±0.10(Predicted) | | form | Solid |
| | SGI-1776 Usage And Synthesis |
| Uses | A novel, ATP competitive inhibitor of Pim1, Pim2 and Pim3 with IC50s of 7 nM, 363 nM and 69 nM, respectively. | | Uses | SGI-1776 is a Pim-1 kinase inhibitor. Potent PIM inhibitor. | | Definition | ChEBI: N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-6-imidazo[1,2-b]pyridazinamine is a member of imidazoles. | | Biological Activity | sgi-1776 free base, n-((1-methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, is a potent atp-competitive inhibitor of the serine/threonine family of pim kinase, an enzyme regulating cell survival. through extensive biomedical characterization, sgi-1776 exhibits specificity to the three isoforms of the pim family, including pim-1, pim-2, and pim-3. according to preliminary results from studies treating prostate cancer cells, sgi-1776 dose-dependently reduces phosphorylation of known pim kinase substrates involved in cell cycle progression and apotosis (p21cip1/waf1 and bad), compromises overall cell viability by inducing g1 cell cycle arrest and triggering apoptosis, and reduces cell viability in a multidrug resistance 1 (mdr1) protein based taxane-refractory prostate cancer cell line.shannon m. mumenthaler, patricia y.b. ng, amanda hodge, davide bearss, gregory berk, sarath kanekal, sanjeev redkar, pietro taverna, davide b. agus, and anjali jain. pharmacological inhibition of pim kinases alters prostate cancer cell growth and resensitizes chemoresistant cells to taxanes. mol cancer ther. 2009; 8(10): 2882-2893lisa s. chen, s anjeev redkar, david bearss, william g. wierda and varsha gandhi. pim kinase inhibitor, sgi-1776, induces apoptosis in cll lymphocytes. blood. 2009; 114(19): 4150-4157 | | target | Pim1 |
| | SGI-1776 Preparation Products And Raw materials |
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