GNE-9822

GNE-9822 is a potent, orally active and selective ITK inhibitor with a Ki value of 0.7 nM. GNE-9822 has good ADME properties. GNE-9822 can be used in research of asthma[1].

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Itk

GNE-9822 (compound 28) 抑制 PLCγ 的磷酸化，IC50 值为 55 nM[1]。

GNE-9822 (compound 28; po and iv; 1 and 5 mg/kg) 在小鼠和大鼠中观察到良好的生物利用度和半衰期[1]。 Animal Model: BALB/c mouse and Sprague-Dawley rats[1] Dosage: 1 and 5 mg/kg Administration: po (5 mg/kg) and iv (1 mg/kg) Result: 1.19 species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F mouse (BALB/c) IV 1.0 1.0 1.5 40 2.9 10 mouse (BALB/c) PO 5.0 50 3.8 2.7 36 Animal Model: BALB/c mouse and Sprague-Dawley rats[1] Dosage: 1 and 5 mg/kg Administration: po (5 mg/kg) and iv (1 mg/kg) Result: 1.19 species route dose volume (mL/kg) dose (mg/kg) Cmax (μM) AUC (μM·h) Cl (mL/min/kg) T1/2 (h) Vss (L/kg) %F rat (Sprague-Dawley IV 1.0 1.0 0.6 70 3.0 14 rat (Sprague-Dawley PO 2.0 5.0 0.2 1.1 40

[1]. Burch JD, et, al. Property- and structure-guided discovery of a tetrahydroindazole series of interleukin-2 inducible T-cell kinase inhibitors. J Med Chem. 2014 Jul 10;57(13):5714-27.