SGI-1776 free base

Catalog #
27651-1
$155 *
Size: 5 mg
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Description

SGI-1776 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. Treatment with SGI-1776 induces apoptosis in CLL primary cell line.

Synonyms
N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
Product Info
Storage and Usage
Citations
Purity

≥98% by HPLC

Target(s)
Pim1
Formula
C20H22F3N5O
MW
405.4 Da
Solubility
Soluble in DMSO
Biological Activity
SGI-1776 inhibits Pim1, Pim2, Pim3, and FLT3 with IC50 values of 7 nM, 363 nM, 69 nM, and 44nM respectively.
CAS Registry #
1025065-69-3
Background
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.
References
1. Mumenthaler, SM., et al. Mol Cancer Ther. 2009; 8(10): 2882-2893.
2. Lisa S. Chen, LS et al. Blood. 2009; 114(19): 4150-4157.