Description
JNJ 26854165 (Serdemetan) is a HDM2 inhibitor.
Storage
2 years at -20 centigrade
Molecular Formula
C21H20N4
Chemical Name
N1-(2-(1H-indol-3-yl)ethyl)-N4-(pyridin-4-yl)benzene-1,4-diamine
Solubility
DSMO 66 mg/mL Water
In vitro
JNJ 26854165 inhibits cell growth and induces apoptosis in leukemia cell lines with IC50 values of 0.24, 0.33, 0.32 and 0.44 uM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells. JNJ 26854165 is an oral Mdm2 inhibitor which can inhibit the interaction of Mdm2-p53 complex with the proteasome and increase p53 levels by binding to RING domain of Mdm2.
In vivo
JNJ 26854165 leads to significant differences in EFS distribution in 17 of the 36 (47%) evaluable solid tumor xenografts and in 5 of 7 (71%) of the evaluable ALL xenografts using a dose of 20 mg/kg administered via oral gavage daily for 5 days, repeated for 6 weeks
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