Serdemetan (JNJ-26854165)

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.

CAS No. 881202-45-5

サイズ	価格(税別)	在庫状況
5mg	JPY 20200	国内在庫あり
25mg	JPY 63400	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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カスタマーフィードバック6个实验数据

製品安全説明書

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Serdemetan (JNJ-26854165)関連製品

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シグナル伝達経路

p53シグナル伝達経路

p53阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報	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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

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.

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]
細胞実験	細胞株	OCI-AML-3, MOLM-13, NB4 and U937 cells
	濃度	0-10 μM
	反応時間	72 hours
	実験の流れ	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
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	Bcr-abl / p-Bcr-abl / p-CrkL / STAT5 / p-STAT5 / STAT3 / p-STAT3 MDM2 / p-MDM2 / p53 ABCA1 / ABCG1 / NPC1 / NPC2 / HMGcoR p53 / HDM2 / HDMX / p21 / Noxa / Puma		27999193
	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]
動物実験	動物モデル	CB17SC scid^-/- female mice.
	投与量	≤20 mg/kg
	投与経路	Administered via p.o.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT00676910	Completed	Neoplasms	Johnson & Johnson Pharmaceutical Research & Development L.L.C.	November 2006	Phase 1

参考
[1] Kojima K, et al. Mol Cancer Ther. 2010, 9(9), 2545-2557. [2] Yuan Y, et al. J Hematol Oncol. 2011, 4:16. [3] Chargari C, et al. Cancer Lett. 2011, 312(2), 209-218. [4] Smith MA, et al. Pediatr Blood Cancer, 2012, 59(2), 329-332. + 展開

参考

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

+ 展開

化学情報

分子量	328.41	化学式	C₂₁H₂₀N₄
CAS No.	881202-45-5	SDF	Download Serdemetan (JNJ-26854165) SDFをダウンロードする
Smiles	C1=CC=C2C(=C1)C(=CN2)CCNC3=CC=C(C=C3)NC4=CC=NC=C4
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 66 mg/mL ( (200.96 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 2 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):