Navtemadlin

SKU: orb1296183

Description

Navtemadlin (AMG-232) is a highly potent and selective oral inhibitor of the p53-MDM2 interaction, exhibiting an IC50 of 0.6 nM and a Kd of 0.045 nM for MDM2. It is widely used in cancer research to reactivate p53 pathways, demonstrating antitumor efficacy in both in vitro cellular assays and in vivo xenograft models.

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1352066-68-2
• MW: 568.55
• Purity: 99.08% (May vary between batches)
• Formula: C₂₈H₃₅Cl₂NO₅S
• SMILES: CC(C)[C@@H](CS(=O)(=O)C(C)C)N1[C@@H]([C@H](C[C@](C)(CC(O)=O)C1=O)c1cccc(Cl)c1)c1ccc(Cl)cc1
• Target: Mdm2,MDM-2/p53,E1/E2/E3 Enzyme
• Solubility: DMSO:150 mg/mL (263.83 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.52 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  MDM2:0.045 nM (Kd)|p53-MDM2:0.6 nM
• In Vivo:
  METHODS: Navtemadlin (AMG232)(20 mg/kg (ip)) was used to treat C57Bl/6 mice bearing B16-F10 melanoma tumors to observe whether it inhibited tumor growth in mice. RESULTS When Navtemadlin (AMG232) was administered daily starting from day 3, p53 tumor size was reduced by approximately 30%-50%. METHODS: Navtemadlin (AMG232) (10, 25, 75 mg/kg, once daily, orally) was used to observe whether it could inhibit the growth of mouse tumor xenografts. RESULTS Navtemadlin (AMG232) activated p53 pathway activity in vivo and effectively inhibited the growth of mouse tumor xenografts. It also blocked DNA synthesis and induced apoptosis in vivo.
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• In Vitro:
  METHODS: Navtemadlin (0.1, 1, 10 μM) treated B16-F10 cells to determine whether reactivation of p53 by Navtemadlin would induce tumor growth arrest. RESULTS Navtemadlin induced significant p53-dependent growth arrest but minimal apoptosis in B16-F10 cells.
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• Cell Research:
  Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347, and A427 cells. Concentration: 0-10 μM . Incubation Time: 72 hours.
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• Animal Research:
  Animal Model: Female athymic nude mice (n=10) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage .

Storage & Handling

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

Alternative Names

Ubiquitin ligase, Ubiquitin conjugating enzyme, Ubiquitin activating enzyme, AMG232, AMG-232, AMG 232, CS1300, CS-1300, CS 1300, E2 Enzyme, E2 conjugating enzyme, E1Enzyme, E1/E2/E3 Enzyme, E1 activating enzyme, E1 Enzyme, E2Enzyme, E3 Enzyme, MDM-2/p53, MDM2, Inhibitor, E3Enzyme, E3 ligating enzyme, KRT 232, KRT232, KRT-232, inhibit, p53-MDM2, Navtemadlin

Compound Identifiers

PubChem CID

58573469