Formulation: A solid
Formal Name: N-(4-(4-(2-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-2-oxoethoxy)piperidin-1-yl)-2-methoxyphenyl)-6-(1H-pyrazol-3-yl)picolinamide
Purity: ≥98%
Formula Markup: C46H55N9O7S
Formula Weight: 878,1
Shelf life (days): 1460
CAS Number: 2597343-08-1
Notes: JNJ-1013 is a proteolysis-targeting chimera (PROTAC) containing the IL-1 receptor-associated kinase 1 (IRAK1) and IRAK4 inhibitor JH-I-25 and a methylated derivative of the PROTAC building block VH 032 (Item No. 39982).{49930} It degrades IRAK1 with a half-maximal degradation concentration (DC50) value of 3.3 nM in HBL-1 diffuse large B cell lymphoma (DLBCL) cells and is selective for IRAK1 over 7,548 proteins but does degrade cyclin G-associated kinase (GAK) and NmrA-like family domain-containing protein 1 (NMRAL1) at 1 µM. JNJ-1013 (0.3-1 µM) decreases phosphorylated levels of IκBα and STAT3 in HBL-1 cells. It reduces the proliferation of HBL-1 and OCI-LY10 DLBCL cells (IC50s = 60 and 170 nM, respectively).
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