Nelfinavir |
Catalog No.GC17709
One-Click Copy Product Info
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Nelfinavir is a selective, nonpeptidic competitive inhibitor of HIV-1 protease. Nelfinavir shows good in vitro activity against HIV-1 strains.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 159989-64-7
Sample solution is provided at 25 µL, 10mM.
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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.
| 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: | |
| Cas No. | 159989-64-7 | SDF | |
| Chemical 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 | ||
| Canonical SMILES | CC1=C(C=CC=C1O)C(=O)NC(CSC2=CC=CC=C2)C(CN3CC4CCCCC4CC3C(=O)NC(C)(C)C)O | ||
| Formula | C32H45N3O4S | M.Wt | 567.78 |
| Solubility | ≥ 20.45mg/mL in Ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7612 mL | 8.8062 mL | 17.6125 mL |
| 5 mM | 352.2 μL | 1.7612 mL | 3.5225 mL |
| 10 mM | 176.1 μL | 880.6 μL | 1.7612 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)