Shelf life (days): 1460.0
Formulation: A solid
Formal Name: N-[3-(difluoromethyl)-1-[trans-4-[[4-[[3-[1-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-3-methyl-2-oxo-1H-benzimidazol-4-yl]-2-propyn-1-yl]oxy]-1-piperidinyl]methyl]cyclohexyl]-1H-pyrazol-4-yl]-5-(1R,4R)-2-oxa-5-azabicyclo[2.2.1]hept-5-yl-pyrazolo[1,5-a]pyrimidine-3-carboxamide
Purity: ≥95%
Formula Markup: C44H49F2N11O6
Formula Weight: 865.927206
CAS Number: 2432994-31-3
Notes: A PROTAC that drives IRAK4 degradation; induces the degradation of IRAK4 in primary mouse and rat splenocytes and isolated dog, monkey, and human PBMCs (DC50s = 4.2, 2.1, 9.2, 2.9, and 1.5 nM, respectively); selective for IRAK4 over a panel of 468 kinases at 1 µM; inhibits R-848-induced IL-8 release in isolated human PBMCs (IC50 = 3 nM); decreases ear thickness in a mouse model of imiquimod-induced psoriasis at 30 and 100 mg/kg, p.o.
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