SGI-1776 free basePim kinase inhibitor,ATP-competitive CAS# 1025065-69-3 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 1025065-69-3 | SDF | Download SDF |
| PubChem ID | 24795070 | Appearance | Powder |
| Formula | C20H22F3N5O | M.Wt | 405.42 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : 125 mg/mL (308.32 mM; Need ultrasonic) | ||
| Chemical Name | N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine | ||
| SMILES | CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2 | ||
| Standard InChIKey | MHXGEROHKGDZGO-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C20H22F3N5O/c1-27-9-7-14(8-10-27)12-24-18-5-6-19-25-13-17(28(19)26-18)15-3-2-4-16(11-15)29-20(21,22)23/h2-6,11,13-14H,7-10,12H2,1H3,(H,24,26) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM, 50- and 10-fold selective versus Pim2 and Pim3. | ||||||
| Targets | Pim1 | Pim2 | Pim3 | FLT3 | |||
| IC50 | 7 nM | 363 nM | 69 nM | 44nM | |||
| Cell experiment: [1] | |
| Cell lines | Primary lymphocytes from patients with CLL |
| Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
| Reacting condition | 10 μM, 24 hours |
| Applications | In vitro incubation of primary CLL cells with 1, 3, and 10 μM SGI-1776 for 24 hours resulted in an average increase in apoptosis of 10%, 22%, and 38%, respectively, compared with untreated cells. Incubation of CLL cells with SGI-1776 for 48 or 72 hours further increased the percentage of apoptotic cells. |
| Animal experiment: [2] | |
| Animal models | Female BALB/c nude mice bearing 786-O or Caki-1 xenografts |
| Dosage form | Oral administration, 200 mg/kg, once every 5 days, for 3 weeks |
| Application | Treatment with SGI-1776 resulted in a significant decrease in mean tumor volume in both xenograft models compared with the vehicle-treated controls. Besides that, SGI-1776 induced a reduction in Bad phosphorylation without altering total Bad protein levels. It also induced moderate levels of apoptosis. |
| Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| References: [1] Chen L S, Redkar S, Bearss D, et al. Pim kinase inhibitor, SGI-1776, induces apoptosis in chronic lymphocytic leukemia cells. Blood, 2009, 114(19): 4150-4157. [2] Mahalingam D, Espitia C M, Medina E C, et al. Targeting PIM kinase enhances the activity of sunitinib in renal cell carcinoma. British journal of cancer, 2011, 105(10): 1563-1573. | |
SGI-1776 free base Dilution Calculator
SGI-1776 free base Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.4666 mL | 12.3329 mL | 24.6658 mL | 49.3316 mL | 61.6644 mL |
| 5 mM | 0.4933 mL | 2.4666 mL | 4.9332 mL | 9.8663 mL | 12.3329 mL |
| 10 mM | 0.2467 mL | 1.2333 mL | 2.4666 mL | 4.9332 mL | 6.1664 mL |
| 50 mM | 0.0493 mL | 0.2467 mL | 0.4933 mL | 0.9866 mL | 1.2333 mL |
| 100 mM | 0.0247 mL | 0.1233 mL | 0.2467 mL | 0.4933 mL | 0.6166 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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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.
Reference
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): 2882-2893
Lisa 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
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