Details
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)
Molecular Formula | C21H20N4 |
Molecular Weight | 328.4103 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/21922647Curator's Comment: Description was created based on several sources, including
http://www.eurodiagnostico.com/media/pdf/JNJ%2026854165%20(Serdemetan).pdf
http://adisinsight.springer.com/drugs/800014298
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21922647
Curator's Comment: Description was created based on several sources, including
http://www.eurodiagnostico.com/media/pdf/JNJ%2026854165%20(Serdemetan).pdf
http://adisinsight.springer.com/drugs/800014298
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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
yes [IC50 0.4772 uM] | ||||
yes [IC50 2.6837 uM] | ||||
yes [IC50 3.7908 uM] |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21831953
The maximum tolerated dose (MTD) of serdemetan was determined to be 350 mg once daily.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23820125
Serdemetan induced a dose-dependent inhibition of proliferation in both wild-type (wt) and mutant (mut) p53 cell lines, with IC50 values from 0.25 to 3 uM/L, in association with an S phase cell cycle arrest.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 17:15:33 GMT 2023
by
admin
on
Fri Dec 15 17:15:33 GMT 2023
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Record UNII |
ID6YB4W3V8
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Record Status |
Validated (UNII)
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Record Version |
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C129839
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TARGET -> INHIBITOR |
BINDING
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ACTIVE MOIETY |