PX-478 2HCl

For research use only.

Catalog No.S7612

36 publications

PX-478 2HCl Chemical Structure

CAS No. 685898-44-6

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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Selleck's PX-478 2HCl has been cited by 36 publications

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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.
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 NXzmU2V5TnWwY4Tpc44h[XO|YYm= Mn:0NVDjiIoQvF2= M3mz[|I1KGh? MX7zeZBxemW|czDITWYuOc7zIHX4dJJme3Orb36= MoPVN|A1Pzl|M{[=
H460 MVfGeY5kfGmxbjDhd5NigQ>? NFLMb4QyOOLCid88US=> NXL0TWVbemWmdXPl[EBodHWlb4PlJJVxfGGtZTDhcoQhdGGldHH0[UBxem:mdXP0bY9vKHKjdHW= NIjNOos{ODF{OECzOS=>
A549 MkD5SpVv[3Srb36gZZN{[Xl? MojwNVDjiIoQvF2= Ml\GdoVlfWOnZDDncJVkd3OnIIXweIFs\SCjbnSgcIFkfGG2ZTDwdo9lfWO2aX;uJJJifGV? M4D6flMxOTJ6MEO1
SMMC7721 NInjVWJHfW6ldHnvckBie3OjeR?= NGjnZnAzPSEQvF2= NUnmco17OjRiaB?= MkTNbY5pcWKrdIOgcYloemG2aX;uJI9nKFOPTVO3O|Iy NHzJPGEzQTR7NUO4NC=>
EC9706 MnXKSpVv[3Srb36gZZN{[Xl? MlTHNlAh|ryP MVHQXE01PzhiaX7obYJqfGWmIH7vdo1wgGmlIHHu[EBpgXCxeHnhMYlv\HWlZXSgTGlHNTIQsTDlfJBz\XO|aX;uJIF{KHenbHygZZMhS0:[LUKgZY5lKFCGLVyxJIV5eHKnc4Ppc44> NX3WeVE3Ojh3NkCwOlc>
EC109 NIfkXFVHfW6ldHnvckBie3OjeR?= Mom3NlAh|ryP MYjQXE01PzhiaX7obYJqfGWmIH7vdo1wgGmlIHHu[EBpgXCxeHnhMYlv\HWlZXSgTGlHNTIQsTDlfJBz\XO|aX;uJIF{KHenbHygZZMhS0:[LUKgZY5lKFCGLVyxJIV5eHKnc4Ppc44> MVOyPFU3ODB4Nx?=
Tca8113 M3uyTGZ2dmO2aX;uJIF{e2G7 NIjIXXYxNCB3LDDhcoQhOjYkgJpOwG0> NX;VUpB7OjRiaB?= MXry[YR2[2W|IHPlcIx2dGG{IHH1eI9xcGGpeR?= M4iyZlI3PjRyM{G2
PDAC cell lines NV7nNoloTnWwY4Tpc44h[XO|YYm= MUSyOUDPxE1? M4nUfFI1KGh? MoHIbY5lfWOnZDDhJJRz[W6|bH;jZZRqd25ib3[gTG1ISjFiZoLvcUB1cGViboXjcIV2eyC2bzD0bIUh[3m2b4DsZZNu NUDvRms2OjV3NES3O|A>
PC3 NWHMVlFUTnWwY4Tpc44h[XO|YYm= NIDhTnIzOCCqch?= Mo\ITWM2OCCob4KgTGlHNTIQsTDpcohq[mm2aX;uJIZweiCSQ{OgZ4VtdHNidX7k[ZIhdm:{bX;4bYMh[2:wZHn0bY9vKHejczCyNE0zPSEQvH3vcE9N MlnnNVg4OjlzOUK=
DU 145 MnzzSpVv[3Srb36gZZN{[Xl? MoTKNlAhcHJ? MXPJR|UxKG[xcjDITWYuOc7zIHnubIljcXSrb36g[o9zKHSqZTDEWUAyPDViY3XscJMhf2G|II60NE02OCEQvH3vcE9N M2fURVE5PzJ7MUmy

... 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

* 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 C1=CC(=CC=C1CC(C(=O)O)N)[N+](CCCl)(CCCl)[O-].Cl.Cl

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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.|Seattle Genetics Inc. August 2007 Phase 1

Tech Support

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HIF Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID