PIM-KINASE INHIBITOR X CX-6 1PC X 10MG (C005B-229264)

General description

An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC₅₀ = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; K_i = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC₈₀ >500 nM). Shown to arrest the proliferation of several human cancer cells (IC₅₀ = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser¹¹², 4E-BP1-Ser⁶⁵ and Thr^37/46 with an IC₅₀ of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380) and paclitaxel (Cat. No. 580555) toxicity in PC3 cells.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
PIM Kimases

Reversible: yes

Secondary Target
Flt3

Target IC₅₀: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.

Other Notes

Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135.

Legal Information

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

Molecular Weight: 461.94 (free base basis). Empirical Formula: C₂₆H₂₄ClN₃O₃ · xHCl. Quality Level: 100. Assay: ≥. 99% (HPLC). form: powder. manufacturer/tradename: Calbiochem^®. . storage condition: OK to freeze, desiccated (hygroscopic), protect from light. color: orange. solubility: DMSO: 25 . mg/mL. shipped in: ambient. storage temp.: 2-8°C. SMILES string: O: C(/C1: C/C2: CC: C(C3: CC: CC(C(N4CCCN(C)CC4): O): C3)O2)NC5: C1C: C(Cl)C: C5.[xHCl]. Storage Class Code: 11 - Combustible Solids. WGK: WGK 3. Flash Point(F): Not applicable. Flash Point(C): Not applicable.