| Stereochemistry | ACHIRAL |
| Molecular Formula | C21H20N4 |
| Molecular Weight | 328.4103 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C(CC1=CNC2=C1C=CC=C2)NC3=CC=C(NC4=CC=NC=C4)C=C3
InChI
InChIKey=CEGSUKYESLWKJP-UHFFFAOYSA-N
InChI=1S/C21H20N4/c1-2-4-21-20(3-1)16(15-24-21)9-14-23-17-5-7-18(8-6-17)25-19-10-12-22-13-11-19/h1-8,10-13,15,23-24H,9,14H2,(H,22,25)
JNJ-26854165 (Serdemetan), a novel tryptamine derivative, was developed as an activator of p53, and its initially proposed mechanism of action involved preventing the association of HDM2 with the proteasome and thereby stabilizing HDM2 substrates such as p53. Consistent with this proposed mechanism, Serdemetan induced apoptosis in acute myeloid and lymphoid leukemia cell lines and in primary acute leukemia isolates. Serdemetan is currently being evaluated in Phase I clinical trials in patients with non-small cell lung cancer; prostate cancer; solid tumours.
Approval Year
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
Tox targets
Sourcing
Sample Use Guides
The maximum tolerated dose (MTD) of serdemetan was determined to be 350 mg once daily.
Route of Administration:
Oral
ACTIVE MOIETY
