PX-478 2HCl

For research use only.

Catalog No.S7612

49 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.

Selleck's PX-478 2HCl has been cited by 49 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 NHLsc4lHfW6ldHnvckBie3OjeR?= NYP0SmhOOTEkgJpOwG0> M2nMbFI1KGh? M1;pOZN2eHC{ZYPzJGhKTi1zzsGg[ZhxemW|c3nvci=> NXXVe5RQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C0O|k{OzZpPkOwOFc6OzN4PD;hQi=>
H460 NXTMWXpvTnWwY4Tpc44h[XO|YYm= NEna[3EyOOLCid88US=> M3\yXpJm\HWlZXSg[4x2[2:|ZTD1dJRic2ViYX7kJIxi[3SjdHWgdJJw\HWldHnvckBz[XSn M3vuTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyMUK4NFM2Lz5|MEGyPFA{PTxxYU6=
A549 M2P2[2Z2dmO2aX;uJIF{e2G7 NEPQfoQyOOLCid88US=> M3\KTJJm\HWlZXSg[4x2[2:|ZTD1dJRic2ViYX7kJIxi[3SjdHWgdJJw\HWldHnvckBz[XSn NXniTmlLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxNlgxOzVpPkOwNVI5ODN3PD;hQi=>
SMMC7721 MV3GeY5kfGmxbjDhd5NigQ>? Mn\FNlUh|ryP Mm[3NlQhcA>? M4TCSIlvcGmkaYTzJI1q\3KjdHnvckBw\iCVTV3DO|czOQ>? NWfyUYU{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0PVU{QDBpPkK5OFk2OzhyPD;hQi=>
EC9706 M3HrVGZ2dmO2aX;uJIF{e2G7 NHy2RXEzOCEQvF2= MmH1VHguPDd6IHnubIljcXSnZDDuc5Jud3irYzDhcoQhcHmyb4jpZU1qdmS3Y3XkJGhKTi1zzsGg[ZhxemW|c3nvckBieyC5ZXzsJIF{KEORWD2yJIFv\CCSRD3MNUBmgHC{ZYPzbY9v NGrKRmQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW2NFA3Pyd-Mki1OlAxPjd:L3G+
EC109 M3y4dGZ2dmO2aX;uJIF{e2G7 M17R[FIxKM7:TR?= MYXQXE01PzhiaX7obYJqfGWmIH7vdo1wgGmlIHHu[EBpgXCxeHnhMYlv\HWlZXSgTGlHNTIQsTDlfJBz\XO|aX;uJIF{KHenbHygZZMhS0:[LUKgZY5lKFCGLVyxJIV5eHKnc4Ppc44> MoDBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NkCwOlcoRjJ6NU[wNFY4RC:jPh?=
Tca8113 M2\KVGZ2dmO2aX;uJIF{e2G7 NVvTdHVbOCxiNTygZY5lKDJ34pEJ{txO M2LOdlI1KGh? Ml;5doVlfWOnczDj[YxtfWyjcjDheZRweGijZ4m= MmnqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ4NECzNVYoRjJ4NkSwN|E3RC:jPh?=
PDAC cell lines NIPUUFhHfW6ldHnvckBie3OjeR?= MX[yOUDPxE1? NHfVOW0zPCCq NETTbVRqdmS3Y3XkJIEhfHKjboPsc4NifGmxbjDv[kBJVUeEMTDmdo9uKHSqZTDueYNt\XW|IITvJJRp\SCleYTvdIxie21? MoHwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV3NES3O|AoRjJ3NUS0O|cxRC:jPh?=
PC3 M2fWWGZ2dmO2aX;uJIF{e2G7 M4ix[VIxKGi{ Ml7WTWM2OCCob4KgTGlHNTIQsTDpcohq[mm2aX;uJIZweiCSQ{OgZ4VtdHNidX7k[ZIhdm:{bX;4bYMh[2:wZHn0bY9vKHejczCyNE0zPSEQvH3vcE9N NFqyZpk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEeyPVE6Oid-MUi3NlkyQTJ:L3G+
DU 145 NVO1OmV3TnWwY4Tpc44h[XO|YYm= M3vMVVIxKGi{ Mn6yTWM2OCCob4KgTGlHNTIQsTDpcohq[mm2aX;uJIZweiC2aHWgSHUhOTR3IHPlcIx{KHejczD+OFAuPTBizsztc4wwVA>? MnXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh5MkmxPVIoRjF6N{K5NVkzRC:jPh?=
MCF7 M4P0UmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 Mlv3O|IhcHK| NFnyeGVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiN{KgbJJ{KHWwZHXyJIh6eG:6aXOgZ49v\Gm2aX;uJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDF7Lkeg{txONg>? NEDJVVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKwPVI2Pyd-MkiyNFkzPTd:L3G+
MCF7 NFrafXJHfW6ldHnvckBie3OjeR?= MWCyOEBpenN? NXHwTYFbUW6qaXLpeIlwdiCxZjDITWYuOWGucHjhJEh2dmuwb4fuJI9zcWerbjmgeJJidnOlcnnweIlwdmGuIHHjeIl3cXS7IHX4dJJme3OnZDDpckBpfW2jbjDNR2Y4KGOnbHzzJIFnfGW{IEK0JIhzeyC3bnTldkBpgXCxeHnjJINwdmSrdHnvckBjgSCKUlWgcJVkcW[ncnHz[UBz\XCxcoTldkBo\W6nIHHzd4F6yqBuIFnDOVAhRSB{MD6yJO69VS5? NVP6cpRMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNFkzPTdpPkK4NlA6OjV5PD;hQi=>
MDA-MB-468 MYLBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? Mn\1O|IhcHK| MYDBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[W[2ZYKgO|IhcHK|IIXu[IVzKGi7cH;4bYMh[2:wZHn0bY9vKGK7IF3UWEBie3OjeTygTWM2OCB;IES1MlEh|ryPLh?= MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJyOUK1O{c,Ojh{MEmyOVc9N2F-

... 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 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.|Seagen Inc. August 2007 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID