Serdemetan

SKU: orb1305929

Description

Serdemetan (JNJ-26854165) is an orally active small molecule antagonist of HDM2, which disrupts the p53-HDM2 interaction to reactivate tumor suppression. It has demonstrated antineoplastic activity in preclinical in vitro and in vivo cancer models, supporting its investigation in oncology research.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 881202-45-5
• MW: 328.41
• Purity: 97.13% (May vary between batches)
• Formula: C₂₁H₂₀N₄
• SMILES: C(Cc1c[nH]c2ccccc12)Nc1ccc(Nc2ccncc2)cc1
• Target: p53,E1/E2/E3 Enzyme,MDM-2/p53,Mdm2,Apoptosis
• Solubility: DMSO:50 mg/mL (152.25 mM);Ethanol:2 mg/mL (6.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.09 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  OCI-AML3 cells:0.24 μM|REH cells:0.44 μM|NALM6:0.32 μM|MOLM-13:0.33 μM
• In Vivo:
  In leukemia cell lines, JNJ-26854165 inhibits cell growth and induces apoptosis, demonstrating inhibitory effects on OCI-AML-3 (IC50=0.24 μM), MOLM-13 (IC50=0.33 μM), NALM-6 (IC50=0.32 μM), and REH (IC50=0.44 μM). Additionally, it inhibits cell proliferation in various human cancer cell lines (H460, A549, p53-WT-HCT116, and p53-null-HCT116).
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• In Vitro:
  In both solid and ALL transplant tumor models, oral administration of JNJ-26854165 (20 mg/kg) significantly altered EFS distribution.
• Cell Research:
  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(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

E1 activating enzyme, E1 Enzyme, E1/E2/E3 Enzyme, E1Enzyme, E2 conjugating enzyme, E2 Enzyme, E2Enzyme, E3 Enzyme, Apoptosis, JNJ26854165, JNJ-26854165, JNJ 26854165, inhibit, p53, Inhibitor, HDM2, Mdm2, MDM-2/p53, E3 ligating enzyme, E3Enzyme, Ubiquitin activating enzyme, Ubiquitin conjugating enzyme, Ubiquitin ligase, Serdemetan

Compound Identifiers

PubChem CID

11609586