SerdeMetan
N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine
CAS: 881202-45-5
Molecular Formula: C21H20N4
SerdeMetan - Names and Identifiers
| Name | N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine |
| Synonyms | CS-389 SerdeMetan JNJ 26854165 JNJ26854165 JNJ-26854165 JNJ-26854165 (SerdeMetan) JNJ-26854165 (Serdemetan) N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine JNJ 26854165 N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine JNJ 26854165 JNJ 26854165 N-[2-(1H-Indol-3-yl)ethyl]-N'-(4-pyridinyl)-1,4-benzenediamine |
| CAS | 881202-45-5 |
| EINECS | 200-256-5 |
SerdeMetan - Physico-chemical Properties
| Molecular Formula | C21H20N4 |
| Molar Mass | 328.41 |
| Storage Condition | -20℃ |
| Physical and Chemical Properties | Bioactivity JNJ-26854165 (Serdemetan) is an HDM2 ubiquitin ligase antagonist that acts on p53 wild-type cells to induce early apoptosis, inhibits cell proliferation and delays apoptosis. |
| Target | Target Value p53 (Cell-free assay) HDM2 (Cell-free assay) Mdm2 (Cell-free assay) |
| In vitro study | JNJ-26854165 is a novel B derivative that activates p53 as an HDM2 ubiquitin ligase antagonist. JNJ-26854165 inhibited cell growth and induced apoptosis in leukemia cell lines, and after 72 hours in OCI-AML-3, MOLM-13,NALM-6 and REH cells, IC50 values were 0.24,0.33,0.32 and 0.44 μm, respectively. In addition, JNJ-26854165 acts on cells with p53 mutations, accelerates protease-regulated p21 degradation and transcriptional induction of p21 by anti-p53, induces S-phase delay, and upregulates E2F1 expression, results in preferential apoptosis of S phase cells. JNJ-26854165 is an oral MDM2 inhibitor that inhibits the interaction of the MDM2-p53 complex with proteases and increases p53 levels by binding to the RING domain of MDM2. The latest study shows that JNJ-26854165 acts on four human cancer cell lines: H460,A549,p53-WT-HCT116, and p53-null-HCT116, inhibiting asexual survival. |
| In vivo study | JNJ-26854165, the patient was orally fed 20 mg/kg at a dose of 17 (47%) solid transplanted tumors and 5/7 (71%) ALL transplanted tumors for 5 days for 6 weeks, this resulted in a significant difference in the distribution of EFS. |
SerdeMetan - Risk and Safety
| HS Code | 29339900 |
SerdeMetan - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.045 ml | 15.224 ml | 30.449 ml |
| 5 mM | 0.609 ml | 3.045 ml | 6.09 ml |
| 10 mM | 0.304 ml | 1.522 ml | 3.045 ml |
| 5 mM | 0.061 ml | 0.304 ml | 0.609 ml |
Last Update：2024-01-02 23:10:35
SerdeMetan - Reference Information
| biological activity | JNJ-26854165 (Serdemetan) is an HDM2 ubiquitin ligase antagonist that acts on p53 wild-type cells and induces early apoptosis. In cells lacking functional p53, it inhibits cell proliferation and delays cell apoptosis. |
| target | TargetValue p53 (cell-free say) HDM2 (cell-free say) Mdm2 (cell-free say) |
| Target | Value |
| in vitro study | JNJ-26854165 is a novel tryptamine derivative that activates p53 and acts as an HDM2 ubiquitin ligase antagonist. JNJ-26854165 act on leukemia cell lines, inhibit cell growth and induce apoptosis. After 72 hours of action on OCI-AML-3, MOLM-13,NALM-6 and REH cells, IC50 values are 0.24,0.33,0.32 and 0.44 µM respectively. In addition, JNJ-26854165 acts on cells with p53 mutation, accelerates protease-regulated p21 degradation and anti-p53 transcription induction of p21, induces S-phase delay, and up-regulates E2F1 expression, resulting in preferential apoptosis of S-phase cells. JNJ-26854165 is an oral MDM2 inhibitor, which can inhibit the interaction between MDM2-p53 complex and protease, and increase p53 level by binding with RING domain of MDM2. The latest research shows that JNJ-26854165 acts on four human cancer cell lines: H460,A549,p53-WT-HCT116, and p53-null-HCT116, inhibiting asexual reproduction and survival. |
| in vivo study | JNJ-26854165 were orally fed to 17/36 (47%) solid transplanted tumors and 5/7 (71%) ALL transplanted tumors at a dose of 20 mg/kg for 5 days and repeated for 6 weeks, resulting in obvious differences in EFS distribution. |
Last Update：2024-04-09 21:54:55
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Product Name: JNJ-26854165 (Serdemetan) Visit Supplier Webpage Request for quotationCAS: 881202-45-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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