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
• Empirical Formula (Hill Notation): C₂₀H₂₂F₃N₅O · 2H₂SO₄
• CAS Number: 1173928-26-1
• Molecular Weight: 601.57
• MDL number: MFCD16659064
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• 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

Description

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable