PX-478 2HCl |
| Catalog No.GC11031 |
PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 685898-44-6
Sample solution is provided at 25 µL, 10mM.
PX-478 is a selective inhibitor that suppresses constitutive and hypoxia-induced HIF-1α levels. PX-478 inhibits HIF-1α at multiple levels including inhibition of HIF-1α translation and reduction in HIF-1α mRNA levels.[1] PX-478 also has been shown antitumor activity against several aggressive human tumor xenografts.[2]
In vitro and in vivo study demonstrated that PX-478 could inhibit normoxic and hypoxia-induced HIF-1α expression as well as inflammatory molecule COX-2 and immunosuppressive molecule PD-L1 expression. Therefore, PX-478 shows a wide effect on tumor development, such as suppressing proliferation, promoting cells apoptosis, inhibiting EMT process and arresting cell cycle. In vivo experiment indicated the inhibitory effect of PX-478 on tumor growth. [1]
References:
[1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212.
[2].Palayoor ST, et al. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008 Nov 15;123(10):2430-7.
| Cell experiment [1]: | |
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Cell lines |
EC109 and EC9706 cell lines |
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Preparation Method |
Both cell lines were cultured in RPMI 1640 supplemented with 10% FBS at 37°C in a 5% CO2 humidified incubator. Cells were starved for 24 h in medium containing 0.1% FBS prior to treatment. |
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Reaction Conditions |
PX-478 was added to the cultures to a final concentration of 20 umol/L after serum starvation overnight. |
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Applications |
PX-478 could inhibit normoxic and hypoxia-induced HIF-1α expression as well as COX-2 and PD-L1 expression in vitro at a dose of 20 μM in EC9706 and EC109 cells. Targeted HIF-1α can effectively reduce their expression. |
| Animal experiment [1]: | |
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Animal models |
6-week-old female BALB/c nude mice, 18 ± 2 g, SPF grade |
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Preparation Method |
EC109 cells were re-suspended in PBS at 107/mL. A total of 12 BABL/c nude female mice were used. Mice were injected with EC109 cells in the right flank area to establish the tumor xenograft. The 12 tumor-bearing mice in each group were randomly divided into the control group and the PX-478 groups. All the drugs were delivered via p.o. gavage administration. |
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Dosage form |
30 mg/kg every other day |
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Applications |
PX-478 shows a wide effect on tumor development, such as suppressing proliferation, promoting cells apoptosis, inhibiting EMT process and arresting cell cycle. In vivo mouse xenograft models showed the inhibitory effect on tumor growth. In addition, it can reduce COX-2 and PD-L1 expression. |
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References: [1].Zhu Y, et al. Inhibition of HIF-1α by PX-478 suppresses tumor growth of esophageal squamous cell cancer in vitro and in vivo. Am J Cancer Res. 2017 May 1;7(5):1198-1212. |
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| Cas No. | 685898-44-6 | SDF | |
| Chemical Name | (S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide dihydrochloride | ||
| Canonical SMILES | ClCC[N+](C1=CC=C(C[C@@](N)([H])C(O)=O)C=C1)([O-])CCCl.Cl.Cl | ||
| Formula | C13H20Cl4N2O3 | M.Wt | 394.12 |
| Solubility | 79mg/mL in DMSO (200.45mM), 79mg/mL in Water (200.45mM), 79mg/mL in Ethanol (200.45mM) | Storage | Store at -20°C, stored under nitrogen, away from moisture |
| 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 | 2.5373 mL | 12.6865 mL | 25.373 mL |
| 5 mM | 0.5075 mL | 2.5373 mL | 5.0746 mL |
| 10 mM | 0.2537 mL | 1.2686 mL | 2.5373 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 ddH2O, 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Related Biological Data
Effects of ononin combined with radiation on tumor growth and tumor cell apoptosis in human lung cancer subcutaneous tumor-bearing nude mice model. (D) Representative images of Hematoxylin-eosin (H&E) staining, Ki67 immunohistochemical staining (Scar bars = 40 µm) and TUNEL staining.
PX-478 was purchased from GLPBIO (GC11031, GLPBIO,Montclair, USA),(40mg/kg, 0.2ml, ip).
Phytomedicine 125 (2024): 155290. PMID: 38308918 IF: 7.8996 -
Related Biological Data
(c) Quantitative comparison of the number of CD31+ vessels between TCPS with PX-478 or PBS injection after implantation in FVB mice at 14 d per FOV.
The post-surgery mice were administered of PX478 (100mg kg -1)(GlpBio, USA) in phosphate buffer solution (PBS) every other day for a total of 2 weeks according to Agarwal’s protocol.
J Mater Chem B (2022). PMID: 35971918 IF: 7.5711 -
Related Biological Data
Inhibition of HIF-1α signaling alleviated FA-induced glycolysis in PMs. B, intracellular MGO levels was demonstrated by the mean fluorescence intensity of NAP-DCP-1.
RAW 264.7 cells were pretreated with 30μM PX-478(GlpBio, USA)(a specific HIF-1α inhibitor) for 24h to block HIF-1α signaling.
Chem-Biol Interact 379 (2023): 110514. PMID: 37105513 IF: 5.1 -
Related Biological Data
CM from FA-treated tumor cells and MGO promoted TAM polarization. B, % of M2 TAM measured by CD163+ CD206+ double positive population.
Hela cells were treated with 0, 20, 50μM FA or 50μM FA + 5μM PX-478 (HIF-1α inhibitor)(GlpBio, USA) for 24h.
Toxicol Appl Pharm (2022): 115910. PMID: 35134435 IF: 4.219
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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