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SGI-1776

Chemical Structure : SGI-1776

CAS No.: 1025065-69-3

SGI-1776 (SGI 1776;SGI1776)

Catalog No.: PC-43464Not For Human Use, Lab Use Only.

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

SGI-1776 is a potent, selective, orally active Pim kinase inhibitor with IC50 of 7, 363 and 69 nM for Pim1, Pim2 and Pim3, respectively.
SGI-1776 exhibits promising selectivity against a panel of >300 kinases, shows inhibitory activity against two other kinases: Flt-3 (IC50=44 nM) and Haspin (IC50=34 nM);.
SGI-1776 reduces cell viability of androgen-independent prostate cancer cell lines with IC50 of 2-4 uM, causes cell cycle arrest and caspase-dependent apoptosis in prostate cancer cells, marginally sensitizes prostate cancer cells to taxane-based therapeutics by inhibiting MDR1 activity and inducing apoptosis.
SGI-1776 shows efficacy in xenograft model bearing MV-4-11 tumors.

Physicochemical Properties

M.Wt 405.42
Formula C20H22F3N5O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Imidazo[1,2-b]pyridazin-6-amine, N-[(1-methyl-4-piperidinyl)methyl]-3-[3-(trifluoromethoxy)phenyl]-

References

1. Chen LS, et al. Blood. 2009 Nov 5;114(19):4150-7.

2. Chen LS, et al. Blood. 2011 Jul 21;118(3):693-702.

3. Chang M, et al. Mol Cancer Ther. 2010 Sep;9(9):2478-87.

4. Mumenthaler SM, et al. Mol Cancer Ther. 2009 Oct;8(10):2882-93.

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