PX-478 2HCl

For research use only.

Catalog No.S7612

33 publications

PX-478 2HCl Chemical Structure

Molecular Weight(MW): 394.12

PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

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Selleck's PX-478 2HCl has been cited by 33 publications

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Biological Activity

Description PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.
Targets
HIF-1α [1]
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
TW03-EBV cells MUfGeY5kfGmxbjDhd5NigQ>? MX[xNQKBkc7:TR?= MmDxNlQhcA>? Mlfad5VxeHKnc4OgTGlHNTIQsTDlfJBz\XO|aX;u NV70NoVMOzB2N{mzN|Y>
H460 M4\6dWZ2dmO2aX;uJIF{e2G7 NIfBeZEyOOLCid88US=> NWnTTHFOemWmdXPl[EBodHWlb4PlJJVxfGGtZTDhcoQhdGGldHH0[UBxem:mdXP0bY9vKHKjdHW= NH;yfIQ{ODF{OECzOS=>
A549 NXfue|JVTnWwY4Tpc44h[XO|YYm= MmTvNVDjiIoQvF2= NGnKVmVz\WS3Y3XkJIdtfWOxc3WgeZB1[WunIHHu[EBt[WO2YYTlJJBzd2S3Y4Tpc44hemG2ZR?= MVizNFEzQDB|NR?=
SMMC7721 NY\I[oZ{TnWwY4Tpc44h[XO|YYm= MWSyOUDPxE1? NXzVS4RbOjRiaB?= M1ftbYlvcGmkaYTzJI1q\3KjdHnvckBw\iCVTV3DO|czOQ>? M2XGfVI6PDl3M{iw
EC9706 NViyT4VSTnWwY4Tpc44h[XO|YYm= MUWyNEDPxE1? NXK1Vmp[WFhvNEe4JIlvcGmkaYTl[EBvd3Kvb4jpZ{BidmRiaInwc5hq[S2rbnT1Z4VlKEiLRj2x{tEh\XiycnXzd4lwdiCjczD3[YxtKGG|IFPPXE0zKGGwZDDQSE1NOSCneIDy[ZN{cW:w NHXKfo0zQDV4MEC2Oy=>
EC109 MX7GeY5kfGmxbjDhd5NigQ>? M2nkTVIxKM7:TR?= MX\QXE01PzhiaX7obYJqfGWmIH7vdo1wgGmlIHHu[EBpgXCxeHnhMYlv\HWlZXSgTGlHNTIQsTDlfJBz\XO|aX;uJIF{KHenbHygZZMhS0:[LUKgZY5lKFCGLVyxJIV5eHKnc4Ppc44> NF;STJkzQDV4MEC2Oy=>
Tca8113 MXzGeY5kfGmxbjDhd5NigQ>? MXKwMEA2NCCjbnSgNlXjiIoQvF2= NEj4WIgzPCCq M1jzXJJm\HWlZYOgZ4VtdHWuYYKgZZV1d3CqYXf5 NULrcpozOjZ4NECzNVY>
PDAC cell lines M1;BWmZ2dmO2aX;uJIF{e2G7 M2rrSlI2KM7:TR?= MnLsNlQhcA>? NFTQNlhqdmS3Y3XkJIEhfHKjboPsc4NifGmxbjDv[kBJVUeEMTDmdo9uKHSqZTDueYNt\XW|IITvJJRp\SCleYTvdIxie21? Mle0NlU2PDR5N{C=
PC3 NVjRNIxITnWwY4Tpc44h[XO|YYm= M3jzb|IxKGi{ NXiwXot{UUN3MDDmc5IhUEmILUJOtUBqdmirYnn0bY9vKG[xcjDQR|Mh[2WubIOgeY5l\XJibn;ycY95cWNiY3;u[Il1cW:wIIfhd{AzOC1{NTFOwI1wdC:O NV\MeIRDOTh5MkmxPVI>
DU 145 MnS2SpVv[3Srb36gZZN{[Xl? M2CxeFIxKGi{ MXzJR|UxKG[xcjDITWYuOc7zIHnubIljcXSrb36g[o9zKHSqZTDEWUAyPDViY3XscJMhf2G|II60NE02OCEQvH3vcE9N NF;a[3EyQDd{OUG5Ni=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HIF-1α; 

PubMed: 18729192     


(a) Cells were treated with PX-478 for 20 hr under normoxic condition. 

VEGF / Angiopoietin 1; 

PubMed: 28052321     


Western blot analyses of angiogenic cytokines.

E-cadherin / N-cadherin / Vimentin ; 

PubMed: 28560067     


PX-478 inhibits EMT of ESCC. Expression levels of Vimentin and N-cadherin were decreased while E-cadherin was increased in the PX-478 treatment group.

HIF-1α; 

PubMed: 18729192     


(a) Cells were treated with PX-478 for 20 hr under normoxic condition. 

VEGF / Angiopoietin 1; 

PubMed: 28052321     


Western blot analyses of angiogenic cytokines.

E-cadherin / N-cadherin / Vimentin ; 

PubMed: 28560067     


PX-478 inhibits EMT of ESCC. Expression levels of Vimentin and N-cadherin were decreased while E-cadherin was increased in the PX-478 treatment group.

18729192 28052321 28560067
Growth inhibition assay
Cell viability; 

PubMed: 28052321     


HSCs were treated with PX‐478, cyclopamine or GANT-58 at indicated concentrations for 24 h (A-C, E-G) or 3 h (D). (A) Cell viability was determined using Cell Counting Kit‐8. Data were expressed as percentage of control value (n = 6). *P < 0.05, significantly different from control, Kruskal–Wallis H test. 

Cell viability; 

PubMed: 28052321     


HSCs were treated with PX‐478, cyclopamine or GANT-58 at indicated concentrations for 24 h (A-C, E-G) or 3 h (D). (A) Cell viability was determined using Cell Counting Kit-8. Data were expressed as percentage of control value (n = 6). *P < 0.05, significantly different from control, Kruskal-Wallis H test. 

28052321
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

Animal Research:[1]
- Collapse
  • Animal Models: Mice bearing MCF-7 human breast cancer, HT-29 colon cancer, PC-3 prostate cancer, DU-145 prostate cancer, OvCar-3 ovarian cancer, A-549 non-small cell lung cancer, SHP-77 small cell lung cancer, and Caki-1 renal cancer, Panc-1, MiaPaCa, or BxPC-3 pancreatic cancer xenografts.
  • Dosages: 100 or 120 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 78 mg/mL (197.9 mM)
Water 78 mg/mL (197.9 mM)
Ethanol 78 mg/mL (197.9 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 394.12
Formula

C13H20Cl4N2O3

CAS No. 685898-44-6
Storage powder
in solvent
Synonyms N/A
Smiles Cl.Cl.NC(CC1=CC=C(C=C1)[N+]([O-])(CCCl)CCCl)C(O)=O

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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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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID