GLPBio

Nelfinavir

Catalog No.: GC17709Purity:>99.00%
COASDSData Sheet
Nelfinavir (AG-1341) ist ein potenter und oral bioverfÜgbarer HIV-1-Protease-Inhibitor (Ki=2 nM) fÜr die HIV-Infektion.

Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.

Nelfinavir
Cas No.: 159989-64-7
10mM (in 1mL DMSO)In Stock
$124.00
1
2mgIn Stock
$54.00
1
5mgIn Stock
$99.00
1
10mgIn Stock
$149.00
1
50mgIn Stock
$342.00
1
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Zitate (Citations)

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    632, 686–694 (2024)
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    Nature
    618, 1017–1023 (2023)
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    Nature
    610, 366–372 (2022)
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    Cell
    187(9):2288-2304 (2024)
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    Cell
    183(7):1867-1883 (2020)
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    388(6745) (2025)
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    35, 97–116 (2025)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

Beschreibung (Description)

Nelfinavir is a selective, nonpeptidic competitive inhibitor of HIV-1 protease. Nelfinavir shows good in vitro activity against HIV-1 strains[1].

In vitro, Nelfinavir (1, 2.5, 5, 10, 20, 40 and 60µM; 24 and 48h) dose-dependently suppressed proliferation of human A549 cells[2]. Nelfinavir (20μM; 24h) can directly inhibit the activity of aspartic protease DNA damage inducible 1 homolog 2 (DDI2), thereby effectively blocking the proteolysis of NFE2L1 and enhancing the cytotoxicity of proteasome inhibitors (PIs) in cancer cells[3].

In vivo, combining Nelfinavir (50mg/kg/daily; 13 days; i.p.) with Chloroquine inhibits in vivo growth of human lung cancer xenograft tumors[4]. Nelfinavir (100mg/kg per day; 24 days; i.p.) and metformin, when used in combination, act synergistically to inhibit the growth of cervical cancer cell xenografts in nude mice[5].

References:
[1] Perry CM, Frampton JE, McCormack PL, Siddiqui MA, Cvetković RS. Nelfinavir: a review of its use in the management of HIV infection. Drugs. 2005;65(15):2209-44.
[2] He F, Wang G, Xu Z, Huang Z. Nelfinavir restricts A549 cell growth by inhibiting STAT3 signaling. J Int Med Res. 2021 Jun;49(6):3000605211014989.
[3] Gu Y, Wang X, Wang Y, Wang Y, Li J, Yu FX. Nelfinavir inhibits human DDI2 and potentiates cytotoxicity of proteasome inhibitors. Cell Signal. 2020 Nov;75:109775.
[4] Lopiccolo J, Kawabata S, Gills JJ, Dennis PA. Combining Nelfinavir With Chloroquine Inhibits In Vivo Growth of Human Lung Cancer Xenograft Tumors. In Vivo. 2021 Jan-Feb;35(1):141-145.
[5] Xia C, Chen R, Chen J, Qi Q, Pan Y, Du L, Xiao G, Jiang S. Combining metformin and nelfinavir exhibits synergistic effects against the growth of human cervical cancer cells and xenograft in nude mice. Sci Rep. 2017 Mar 2;7:43373.

Protokoll (Protocol)

Cell experiment [1]:

Cell lines

A549 and H1224

Preparation Method

Human A549 cells were plated in 96-well plates at a density of 8000 cells per well and cultured overnight at 37°C. The next days, cells were treated with different concentrations of Nelfinavir (1, 2.5, 5, 10, 20, 40 and 60µM) for 24 and 48 hours. MTT reagent was added to each well and incubated for 4 hours at 37°C. The formazan crystals formed by the reduction of MTT by mitochondrial succinic dehydrogenase secreted by viable cells were dissolved using 150µL of DMSO. Absorbance was measured at 490nm. The experiment was repeated using H1224 cells.

Reaction Conditions

1, 2.5, 5, 10, 20, 40 and 60µM; 24 and 48 hours

Applications

Nelfinavir dose-dependently suppressed proliferation of human A549 cells.

Animal experiment [2]:

Animal models

6-week-old female athymic NCr-nu/nu mice

Preparation Method

Cells (5×10⁶ H157 or H549) were suspended in 100µL of phosphate-buffered saline and subcutaneously injected into the bilateral rear flanks of 6-week-old female athymic NCr-nu/nu mice. When the transplanted tumors reached a volume of 50mm³, the mice were divided into four groups (5 mice per group): (i) Vehicle control (4% DMSO, 5% polyethylene glycol, 5% Tween 80 in saline); (ii) 50mg/kg Nelfinavir; (iii) 50mg/kg chloroquine; or (iv) the combination of Nelfinavir and chloroquine, with intraperitoneal injection once daily for 13 days. The body weights of the animals and the sizes of the tumors were measured every other day. In all studies, tumor volume was calculated using the formula v=(ab²)/2, where a and b represent the long axis and short axis of the tumor, respectively. Immunoblotting analysis was performed to detect markers of apoptosis and endoplasmic reticulum (ER) stress.

Dosage form

50mg/kg/daily; 13 days; i.p.

Applications

Combining Nelfinavir with Chloroquine inhibits in vivo growth of human lung cancer xenograft tumors

References:
[1] He F, Wang G, Xu Z, Huang Z. Nelfinavir restricts A549 cell growth by inhibiting STAT3 signaling. J Int Med Res. 2021 Jun;49(6):3000605211014989.
[2] Lopiccolo J, Kawabata S, Gills JJ, Dennis PA. Combining Nelfinavir With Chloroquine Inhibits In Vivo Growth of Human Lung Cancer Xenograft Tumors. In Vivo. 2021 Jan-Feb;35(1):141-145.

Produktdokumente (Product Documents)

Purity:>99.00%Appearance:A solid
COASDSData Sheet

Chemische Eigenschaften (Chemical Properties)

CAS-Nr.
159989-64-7
Chemischer Name
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-phenylsulfanylbutyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide
SMILES
CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O
Summenformel
C32H45N3O4S
Molekulargewicht
567.78
Löslichkeit
≥ 20.45mg/mL in Ethanol
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.

Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit

g/mol

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