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.
别名:
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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关于此项目
经验公式（希尔记法）:
C20H22F3N5O · 2H2SO4
化学文摘社编号:
分子量:
601.57
UNSPSC Code:
12352200
MDL number:
产品名称
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.
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
Disclaimer
Toxicity: Standard Handling (A)
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).
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.
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.
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
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