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Serdemetan (JNJ-26854165)

Name: Serdemetan (JNJ-26854165)
Brand: Selleck Chemicals
SKU: S1172
Rating: 5 (14 reviews)

Catalog No.S1172 Purity:99.62%

Serdemetan (JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1.

Serdemetan (JNJ-26854165) Chemical Structure

CAS No. 881202-45-5

Purity & Quality Control

Batch: Purity: 99.62%

99.62

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Signaling Pathway

p53 Signaling Pathway

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
KU-19-19 cell	Growth inhibition assay	Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=0.93236 μM	SANGER
H4 cell	Growth inhibition assay	Inhibition of human H4 cell growth in a cell viability assay, IC50=1.06707 μM	SANGER
KGN cell	Growth inhibition assay	Inhibition of human KGN cell growth in a cell viability assay, IC50=1.6205 μM	SANGER
786-0 cell	Growth inhibition assay	Inhibition of human 786-0 cell growth in a cell viability assay, IC50=1.72989 μM	SANGER
769-P cell	Growth inhibition assay	Inhibition of human 769-P cell growth in a cell viability assay, IC50=1.82224 μM	SANGER
K5 cell	Growth inhibition assay	Inhibition of human K5 cell growth in a cell viability assay, IC50=2.01624 μM	SANGER
MLMA cell	Growth inhibition assay	Inhibition of human KOSC-2 cell growth in a cell viability assay, IC50=2.03217 μM	SANGER
MLMA cell	Growth inhibition assay	Inhibition of human MLMA cell growth in a cell viability assay, IC50=2.28703 μM	SANGER
EW-7 cell	Growth inhibition assay	Inhibition of human EW-7 cell growth in a cell viability assay, IC50=2.32695 μM	SANGER
SW1088 cell	Growth inhibition assay	Inhibition of human SW1088 cell growth in a cell viability assay, IC50=2.80651 μM	SANGER
MC-IXC cell	Growth inhibition assay	Inhibition of human MC-IXC cell growth in a cell viability assay, IC50=2.87792 μM	SANGER
NCI-H2052 cell	Growth inhibition assay	Inhibition of human NCI-H2052 cell growth in a cell viability assay, IC50=3.08157 μM	SANGER
IGR-1 cell	Growth inhibition assay	Inhibition of human IGR-1 cell growth in a cell viability assay, IC50=3.12028 μM	SANGER
DSH1 cell	Growth inhibition assay	Inhibition of human DSH1 cell growth in a cell viability assay, IC50=3.24296 μM	SANGER
PA-1 cell	Growth inhibition assay	Inhibition of human PA-1 cell growth in a cell viability assay, IC50=3.30059μM	SANGER
SK-MEL-3 cell	Growth inhibition assay	Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=3.31207 μM	SANGER
SW900 cell	Growth inhibition assay	Inhibition of human SW900 cell growth in a cell viability assay, IC50=3.48255 μM	SANGER
CAKI-1 cell	Growth inhibition assay	Inhibition of human CAKI-1 cell growth in a cell viability assay, IC50=3.52738 μM	SANGER
ES1 cell	Growth inhibition assay	Inhibition of human ES1 cell growth in a cell viability assay, IC50=3.52897 μM	SANGER
SK-N-DZ cell	Growth inhibition assay	Inhibition of human SK-N-DZ cell growth in a cell viability assay, IC50=3.62595 μM	SANGER
RH-1 cell	Growth inhibition assay	Inhibition of human RH-1 cell growth in a cell viability assay, IC50=3.68463 μM	SANGER
ES8 cell	Growth inhibition assay	Inhibition of human ES8 cell growth in a cell viability assay, IC50=3.69702 μM	SANGER
NEC8 cell	Growth inhibition assay	Inhibition of human NEC8 cell growth in a cell viability assay, IC50=3.76982 μM	SANGER
LNCaP-Clone-FGC cell	Growth inhibition assay	Inhibition of human LNCaP-Clone-FGC cell growth in a cell viability assay, IC50=3.83536 μM	SANGER
HCE-4 cell	Growth inhibition assay	Inhibition of human HCE-4 cell growth in a cell viability assay, IC50=3.9807 μM	SANGER
U-118-MG cell	Growth inhibition assay	Inhibition of human U-118-MG cell growth in a cell viability assay, IC50=4.01066 μM	SANGER
GI-ME-N cell	Growth inhibition assay	Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=4.08796 μM	SANGER
LB1047-RCC cell	Growth inhibition assay	Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=4.16143 μM	SANGER
HT-1080 cell	Growth inhibition assay	Inhibition of human HT-1080 cell growth in a cell viability assay, IC50=4.19921 μM	SANGER
NB69 cell	Growth inhibition assay	Inhibition of human NB69 cell growth in a cell viability assay, IC50=4.35047 μM	SANGER
NCI-H1693 cell	Growth inhibition assay	Inhibition of human NCI-H1693 cell growth in a cell viability assay, IC50=4.44895 μM	SANGER
HSC-3 cell	Growth inhibition assay	Inhibition of human HSC-3 cell growth in a cell viability assay, IC50=4.49933 μM	SANGER
MDA-MB-231 cell	Growth inhibition assay	Inhibition of human MDA-MB-231 cell growth in a cell viability assay, IC50=4.55899 μM	SANGER
HOS cell	Growth inhibition assay	Inhibition of human HOS cell growth in a cell viability assay, IC50=4.7863 μM	SANGER
BT-549 cell	Growth inhibition assay	Inhibition of human BT-549 cell growth in a cell viability assay, IC50=4.7887 μM	SANGER
NB17 cell	Growth inhibition assay	Inhibition of human NB17 cell growth in a cell viability assay, IC50=4.78976 μM	SANGER
5637 cell	Growth inhibition assay	Inhibition of human 5637 cell growth in a cell viability assay, IC50=4.79652 μM	SANGER
OVCAR-8 cell	Growth inhibition assay	Inhibition of human OVCAR-8 cell growth in a cell viability assay, IC50=4.92436 μM	SANGER
G-402 cell	Growth inhibition assay	Inhibition of human G-402 cell growth in a cell viability assay, IC50=4.93035 μM	SANGER
BB30-HNC cell	Growth inhibition assay	Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=5.07218 μM	SANGER
HCC1806 cell	Growth inhibition assay	Inhibition of human HCC1806 cell growth in a cell viability assay, IC50=5.08339 μM	SANGER
COLO-800 cell	Growth inhibition assay	Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=5.1264 μM	SANGER
FADU cell	Growth inhibition assay	Inhibition of human FADU cell growth in a cell viability assay, IC50=5.36557 μM	SANGER
NCI-H1651 cell	Growth inhibition assay	Inhibition of human NCI-H1651 cell growth in a cell viability assay, IC50=5.39409 μM	SANGER
AGS cell	Growth inhibition assay	Inhibition of human AGS cell growth in a cell viability assay, IC50=5.47711 μM	SANGER
CHP-212 cell	Growth inhibition assay	Inhibition of human CHP-212 cell growth in a cell viability assay, IC50=5.39409 μM	SANGER
YAPC cell	Growth inhibition assay	Inhibition of human YAPC cell growth in a cell viability assay, IC50=5.47711 μM	SANGER
GOTO cell	Growth inhibition assay	Inhibition of human GOTO cell growth in a cell viability assay, IC50=5.49576 μM	SANGER
KYSE-510 cell	Growth inhibition assay	Inhibition of human KYSE-510 cell growth in a cell viability assay, IC50=5.511 μM	SANGER
NCI-H2342 cell	Growth inhibition assay	Inhibition of human NCI-H2342 cell growth in a cell viability assay, IC50=5.53278 μM	SANGER
BFTC-905 cell	Growth inhibition assay	Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=5.62835 μM	SANGER
EW-16 cell	Growth inhibition assay	Inhibition of human EW-16 cell growth in a cell viability assay, IC50=5.72093 μM	SANGER
SK-MEL-30 cell	Growth inhibition assay	Inhibition of human SK-MEL-30 cell growth in a cell viability assay, IC50=5.74543 μM	SANGER
HLE cell	Growth inhibition assay	Inhibition of human HLE cell growth in a cell viability assay, IC50=5.77489 μM	SANGER
T98G cell	Growth inhibition assay	Inhibition of human T98G cell growth in a cell viability assay, IC50=5.79635 μM	SANGER
HUTU-80 cell	Growth inhibition assay	Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=5.84228 μM	SANGER
NOS-1 cell	Growth inhibition assay	Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=5.94766 μM	SANGER
SW780 cell	Growth inhibition assay	Inhibition of human SW780 cell growth in a cell viability assay, IC50=5.96949 μM	SANGER
KYSE-180 cell	Growth inhibition assay	Inhibition of human KYSE-180 cell growth in a cell viability assay, IC50=5.97654 μM	SANGER
MDA-MB-361 cell	Growth inhibition assay	Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=5.98647 μM	SANGER
SNU-C2B cell	Growth inhibition assay	Inhibition of human SNU-C2B cell growth in a cell viability assay, IC50=6.01138 μM	SANGER
NCI-H661 cell	Growth inhibition assay	Inhibition of human NCI-H661 cell growth in a cell viability assay, IC50=6.0694 μM	SANGER
OE33 cell	Growth inhibition assay	Inhibition of human OE33 cell growth in a cell viability assay, IC50=6.14389 μM	SANGER
TYK-nu cell	Growth inhibition assay	Inhibition of human TYK-nu cell growth in a cell viability assay, IC50=6.21863 μM	SANGER
COLO-792 cell	Growth inhibition assay	Inhibition of human COLO-792 cell growth in a cell viability assay, IC50=6.25219 μM	SANGER
HEL cell	Growth inhibition assay	Inhibition of human HEL cell growth in a cell viability assay, IC50=6.2676 μM	SANGER
D-566MG cell	Growth inhibition assay	Inhibition of human D-566MG cell growth in a cell viability assay, IC50=6.33491 μM	SANGER
U031 cell	Growth inhibition assay	Inhibition of human U031 cell growth in a cell viability assay, IC50=6.41816 μM	SANGER
COR-L23 cell	Growth inhibition assay	Inhibition of human COR-L23 cell growth in a cell viability assay, IC50=6.43346 μM	SANGER
NCI-H2452 cell	Growth inhibition assay	Inhibition of human NCI-H2452 cell growth in a cell viability assay, IC50=6.52281 μM	SANGER
BB65-RCC cell	Growth inhibition assay	Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=6.6459 μM	SANGER
CAL-33 cell	Growth inhibition assay	Inhibition of human CAL-33 cell growth in a cell viability assay, IC50=6.65665 μM	SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description

Targets

p53 ^[1]
(Cell-free assay)

HDM2 ^[1]
(Cell-free assay)

Mdm2 ^[2]
(Cell-free assay)

In vitro
In vitro	JNJ 26854165 is a novel tryptamine derivative which activates p53 and acts as a HDM2 ubiquitin ligase antagonist. 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 μM at 72 hours for OCI-AML-3, MOLM-13, NALM-6 and REH cells, respectively. In addition, JNJ 26854165 accelerates proteasome-mediated degradation of p21 and antagonizes the transcriptional induction of p21 by p53. It also induces S-phase delay and upregulates E2F1 expression in p53 mutant cells, resulting in preferential apoptosis of S-phase cells. ^[1] 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. ^[2] A recent study shows that JNJ 26854165 inhibits clonogenic survival in four human cancer cell lines: H460, A549, p53-WT-HCT116, and p53-null-HCT116. ^[3]
Cell Research	Cell lines	OCI-AML-3, MOLM-13, NB4 and U937 cells
	Concentrations	0-10 μM
	Incubation Time	72 hours
	Method	Cell lines are maintained in RPMI 1640 medium containing 10% heat-inactivated fetal calf serum (FCS). OCI-AML-3, MOLM-13, NB4 and U937 cells are derived from acute myelogenous leukemia (AML) patients, K562 from a chronic myelogenous leukemia (CML) patient in blast crisis, and NALM-6, REH, P12-ICHIK
Experimental Result Images	Methods	Biomarkers	Images	PMID
	Western blot	p53 / HDM2 / HDMX / p21 / Noxa / Puma ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR MDM2 / p-MDM2 / p53 Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3		20736344
	Growth inhibition assay	Cell viability		23820125
	Immunofluorescence	p53		27999193

In Vivo
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. ^[4]
Animal Research	Animal Models	CB17SC scid^-/- female mice.
	Dosages	≤20 mg/kg
	Administration	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00676910	Completed	Neoplasms	Johnson & Johnson Pharmaceutical Research & Development L.L.C.	November 2006	Phase 1

References

[4] Smith MA, et al. Pediatr Blood Cancer, 2012, 59(2), 329-332.

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Chemical Information & Solubility

Molecular Weight	328.41	Formula	C₂₁H₂₀N₄
CAS No.	881202-45-5	SDF	Download Serdemetan (JNJ-26854165) SDF
Smiles	C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 66 mg/mL ( (200.96 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molecular Weight Calculator

In vivo Batch: Add solvents to the product individually and in order.				In vivo Formulation Calculator
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.300mg/ml (10.05mM)	Taking the 1 mL working solution as an example, add 50 μL of 66 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.400mg/ml (1.22mM)	Taking the 1 mL working solution as an example, add 50 μL of 8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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