PIM-Kinase Inhibitor X, CX-6258 - Calbiochem

PIM-Kinase Inhibitor X, CX-6258 - Calbiochem 화학적 특성, 용도, 생산

• 일반 설명

  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

PIM-Kinase Inhibitor X, CX-6258 - Calbiochem 공급 업체

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