SAR405838

SKU: orb1685648

Description

SAR405838

Research Area

Cell Biology, Protein Biochemistry

Key Properties

• CAS Number: 1303607-60-4
• MW: 562.5
• Purity: 98.63%
• Formula: C₂₉H₃₄Cl₂FN₃O₃
• SMILES: CC(C)(C)C[C@@H]1N[C@H]([C@H](c2cccc(Cl)c2F)[C@]11C(=O)Nc2cc(Cl)ccc12)C(=O)N[C@H]1CC[C@H](O)CC1
• Target: E1/E2/E3 Enzyme,Mdm2,Apoptosis,MDM-2/p53
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.87 mM);DMSO:245 mg/mL (435.56 mM);Ethanol:29 mg/mL (51.56 mM)

Bioactivity

• Target IC50:
  MDM2:0.88 nM(Ki)
• In Vivo:
  I the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, SAR405838 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,).
• In Vitro:
  SAR405838 binds to MDM2 with Ki of 0.88 nM. SAR405838 potently inhibits cell growth in cancer cell lines, including SJSA-1 IC50 0.092 μM), RS4;11 IC50 0.089 μM), LNCaP IC50 0.27 μM), and HCT-116 IC50 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 IC50 >10 μM), PC-3 IC50 >10 μM), SW620 IC50 >10 μM), and HCT-116 (p53-/-) IC50 >20 μM) cells.
• Cell Research:
  Cell growth Inhibition activity is determined in a water-soluble tetrazolium-based assay. Cell death is measured by trypan blue staining and apoptosis is determined using an Annexin V-FLUOS staining kit.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

E2 Enzyme, E2Enzyme, E3 Enzyme, E3Enzyme, E1/E2/E3 Enzyme, E1Enzyme, E1 Enzyme, MDM-2/p53, Mdm2, MI 773, MI 77301, MI773, MI-773, MI77301, MI-77301, SAR405838, SAR-405838, SAR 405838

Compound Identifiers

PubChem CID

53476877