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About This Item
Empirical Formula (Hill Notation):
C20H22F3N5O · 2H2SO4
CAS Number:
Molecular Weight:
601.57
MDL number:
UNSPSC Code:
12352200
Quality Level
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
SMILES string
CN(CC1)CCC1CNC(C=C2)=NN3C2=NC=C3C4=CC(OC(F)(F)F)=CC=C4
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.
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 Code
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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