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SGI-1776 free basePim kinase inhibitor,ATP-competitive

SGI-1776 free base

Catalog No. A4192
Size Price Stock Qty
Evaluation Sample $28.00 In stock
5mg $90.00 In stock
10mg $170.00 In stock
50mg $410.00 In stock

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Sample solution is provided at 25 µL, 10mM.

Product Citations

1. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID:25538080

Quality Control

Chemical structure

SGI-1776 free base

Related Biological Data

SGI-1776 free base

Related Biological Data

SGI-1776 free base

Biological Activity

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    

Protocol

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.

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Chemical Properties

Cas No. 1025065-69-3 SDF Download SDF
Synonyms SGI1776,SGI 1776
Chemical Name N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
Canonical SMILES CN1CCC(CC1)CNC2=NN3C(=NC=C3C4=CC(=CC=C4)OC(F)(F)F)C=C2
Formula C20H22F3N5O M.Wt 405.42
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
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.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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Background

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