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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
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Serdemetan (JNJ-26854165)関連製品
シグナル伝達経路
p53阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 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 |
|
| 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 |
|---|---|---|---|---|---|
| NCT00676910 | Completed | Neoplasms |
Johnson & Johnson Pharmaceutical Research & Development L.L.C. |
November 2006 | Phase 1 |
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 | |||
|
In vitro |
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 Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
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）
mg/kg
g
μL
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。
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納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間