Nelfinavir mesylate

SKU: orb1226070

Description

A potent and orally bioavailable HIV-1 protease inhibitor with Ki of 2 nM; exhibits an antiviral EC50 of 30 nM in HIV-1 strain RF-infected CEM-SS cells; also inhibits the proliferation of NSCLC cells, as well as every cell line in the NCI60 cell line panel with mean GI50 of 5.2 uM, induces endoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo.HIV Infection Approved(In Vitro):Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells.Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells.Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines.Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT.Nelfinavir Mesylate activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system.Nelfinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 35.93 μM.(In Vivo):Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice.

Key Properties

• CAS Number: 159989-65-8
• MW: 663.8881
• Purity: >98% (HPLC)
• Formula: C₃₃H₄₉N₃O₇S₂
• SMILES: CC1=C(C=CC=C1O)C(=O)N[C@@H](CSC2=CC=CC=C2)[C@@H](CN3C[C@H]4CCCC[C@H]4C[C@H]3C(=O)NC(C)(C)C)O.CS(=O)(=O)O
• Target: HIV
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  Nelfinavir Mesylate (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice. Animal model: NOD/SCID mice (bearing U266-luc cells). Dosage: 75 mg/kg. Administration: i.p.; 5 days a week for 21 days. Result: Decreased MM cell growth in NOD/SCID mice.
• In Vitro:
  Nelfinavir (AG1341) Mesylate (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells. Nelfinavir Mesylate inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells. Nelfinavir Mesylate (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines. Nelfinavir Mesylate (5 μM; 0-24 hours) decreases the phosphorylation of AKT. Nelfinavir Mesylate activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system. Nelfinavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 35.93 μM. Cell Proliferation Assay Cell line: RPMI, LP1, U266, OPM2 and MM1S cells. Concentration: 1, 2, 5, 10 μM. Incubation time: 48 hours. Result: Inhibited the proliferation of RPMI, LP1, U266, OPM2 and MM1S cell lines in a dose-dependent manner with an IC50 of 1-5 μM. Apoptosis Analysis Cell line: LP1 and U266 cells. Concentration: 1-10 μM. Incubation time: 17 hours. Result: Induced a dose-dependent increase in the percentage of annexin V+/propidium iodide+ cells. Western blot analysis. Cell line: U266 cells. Concentration: 5 μM. Incubation time: 0-24 hours. Result: The level of AKT phosphorylation in U266 cells decreased.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AG-1343 mesylate

Quick Database Links

Gene Symbol

HIV