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PX-478 2HCl
Catalog No.S7612
For research use only.
PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1.
CAS No. 685898-44-6
Selleck's PX-478 2HCl has been cited by 55 publications
Purity & Quality Control
Choose Selective HIF Inhibitors
Related Compound Libraries
Other HIF Products
Biological Activity
| Description | PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. PX-478 2HCl induces apoptosis and has anti-tumor activity. Phase 1. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
PX-478 lowers HIF-1α protein levels and HIF-1 transactivation in hypoxia and in normoxia in a variety of cancer cell lines, but has a more pronounced effect on translation of proteins, such as HIF-1α in hypoxia. [2] PX-478 also enhances the radiosensitivity of prostate carcinoma PC3 cells. [3] |
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| In vivo | In HT-29 human colon cancer xenografts, PX-478 suppresses HIF-1alpha levels and inhibits the expression of HIF-1 target genes including vascular endothelial growth factor and the glucose transporter-1. In addition, PX-478 (100 or 120 mg/kg i.p.) also shows antitumor activity including cures against several established human tumor xenografts that is related to the levels of HIF-1α. [1] In high-fat-diet mice, PX-478 causes reduced fibrosis and fewer inflammatory infiltrates in their adipose tissues. [4] |
Protocol (from reference)
| Animal Research:[1] |
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 394.12 | ||
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| Formula | C13H20Cl4N2O3 |
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| CAS No. | 685898-44-6 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | C1=CC(=CC=C1CC(C(=O)O)N)[N+](CCCl)(CCCl)[O-].Cl.Cl | ||
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT00522652 | Completed | Drug: PX-478 | Advanced Solid Tumors|Lymphoma | Cascadian Therapeutics Inc.|Seagen Inc. | August 2007 | Phase 1 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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