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SGI-1776 free base Data Sheet
| Product Name: | SGI-1776 free base |
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|---|---|---|
| CAS No.: | 1025065-69-3 | |
| Cat. No.: | HY-13287 | |
| MWt: | 405.42 | |
| Formula: | C20H22F3N5O | |
| Purity : | >98% | |
| Solubility: | DMSO : 125 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively.
IC50 & Target:Ki: 7 nM (Pim-1), 363 nM (Pim-2), 69 nM (Pim-3)[4]
In Vitro:SGI-1776 free base (2.5, 5 μM) inhibits Pim-1 protein expression and Pim-1 kinase activity in SACC cells. SGI-1776 free base (2.5, 5 μM) causes cell cycle arrest and reduces cell proliferation in SACC-83 and SACC-LM cells[1]. SGI-1776 free base (5 μM) inhibits cell migration and invasiveness in both SACC-83 and SACC-LM cells. SGI-1776 free base (0, 2.5, or 5 μM) induces apoptosis via Caspase-3 activation[1]. SGI-1776 free base (5 µM) exerts inhibitory effects on both lipid accumulation and TG synthesis without affecting the number of adipocytes[2]. SGI-1776 free base (5 µM) inhibits adipogenesis particularly at an early phase of differentiation[2]. SGI-1776 free base (5 µM) decreases the expression of C/EBP-α and PPAR-γ and the phosphorylation levels of STAT-3 during adipocyte differentiation, and downregulates the protein and/or mRNA expression of FAS, leptin and RANTES during adipocyte differentiation[2]. SGI-1776 free base shows the significant activity against HO-8910 cells in a dose-dependent manner, with IC50 of (5.2±0.6) µM, and the inhibiting effect of SGI-1776 free base is sharply increased from 1.25 µM to 20 µM in vitro[3]. SGI-1776 free base inhibits the migration and invasion of HO-8910 cells in a dose-dependent manner, and the inhibiting migration and invasion rate of 5 µM[3]. SGI-1776 free base (2.5, 5 and 10 µM) decreases Pim-1 kinase activity of HO-8910 cells in a dose-dependent manner. Furthermore, the down-regulation of Pim-1 expression by SGI-1776 free base significantly inhibits cell viability, arrests cell in G1 phase, and inhibits the migration and invasion[3]. In Vivo:SGI-1776 free base (75, 200 mg/kg, p.o.) shows potent and sustained antitumor activity in a dose dependent manner in MV-4-11 xenografts in mice[4]. |
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