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Merck

526528

PIM-Kinase Inhibitor IX, SGI-1776

The PIM-Kinase Inhibitor IX, SGI-1776 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

PIM-Kinase Inhibitor IX, SGI-1776, N-((1-Methylpiperidin-4-yl)methyl)-3-(3-(trifluoromethoxy)phenyl)imidazo[1,2-b]pyridazin-6-amine, 2H2SO4

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About This Item

Empirical Formula (Hill Notation):
C20H22F3N5O · 2H2SO4
CAS Number:
1173928-26-1
Molecular Weight:
601.57
UNSPSC Code:
12352200
MDL number:
MFCD16659064
Assay:
≥99% (HPLC)
Form:
powder
Quality level:
100
Storage condition:
OK to freeze, desiccated (hygroscopic), protect from light

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SMILES string

CN(CC1)CCC1CNC(C=C2)=NN3C2=NC=C3C4=CC(OC(F)(F)F)=CC=C4

assay

≥99% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze, desiccated (hygroscopic), protect from light

color

off-white

solubility

DMSO: 100 mg/mL, clear, nearly colorless, water: 100 mg/mL, clear, nearly colorless

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

General description

A cell-permeable imidazopyridazine compound that acts as a potent, reversible and ATP-competitive inhibitor of Pim-1,2,3, Flt-3 and haspin kinase activities (IC50 = 7, 363, 69, 44 and 34 nM, respectively) with moderate (40% inhibition at 1 µM for c-kit) to excellent selectivity over CDKs, Aurora, Chk1, IKK, JNK, Abl, Raf, PKA, PKC and PI 3-K among 300-kinases. Shown to inhibit RNA synthesis, block phosphorylation of c-Myc-Ser62 and STAT3-Tyr705, and decrease c-Myc and Mcl-1 protein levels; cause cell cycle arrest and induce apoptosis in CLL lymphocytes and in AML cells, and efficiently arrest the growth of several prostate cancer cells (IC50<10 µM).

Packaging

Packaged under inert gas

Preparation Note

Following reconstituion, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Chen, L.S., et al. 2011. Blood118, 693.
Chang, M., et al. 2010. Mol. Cancer Ther.9, 2478.
Mumenthaler, S.M., et al. 2009. Mol. Cancer Ther.8, 2882.
Chen, L.S., et al. 2009. Blood 114, 4150.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class

11 - Combustible Solids

wgk

WGK 2

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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