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.

PX-478 2HCl Chemical Structure

CAS No. 685898-44-6

Selleck's PX-478 2HCl has been cited by 55 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 NXuwXIZmTnWwY4Tpc44h[XO|YYm= NXHpclNXOTEkgJpOwG0> NH3jdlIzPCCq NFn2OHB{fXCycnXzd{BJUUZvMd8xJIV5eHKnc4Ppc44> M1fWZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNEe5N|M3Lz5|MES3PVM{PjxxYU6=
H460 MVHGeY5kfGmxbjDhd5NigQ>? M1G2WlEx6oDLzszN NELCR5Fz\WS3Y3XkJIdtfWOxc3WgeZB1[WunIHHu[EBt[WO2YYTlJJBzd2S3Y4Tpc44hemG2ZR?= MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODF{OECzOUc,OzBzMkiwN|U9N2F-
A549 M1rMT2Z2dmO2aX;uJIF{e2G7 MV:xNQKBkc7:TR?= MnrvdoVlfWOnZDDncJVkd3OnIIXweIFs\SCjbnSgcIFkfGG2ZTDwdo9lfWO2aX;uJJJifGV? NFy5ZY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGyPFA{PSd-M{CxNlgxOzV:L3G+
SMMC7721 MYXGeY5kfGmxbjDhd5NigQ>? MWKyOUDPxE1? NYjWWpdUOjRiaB?= MUHpcohq[mm2czDtbYdz[XSrb36gc4YhW02PQ{e3NlE> MlnxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2OUWzPFAoRjJ7NEm1N|gxRC:jPh?=
EC9706 M{\Gb2Z2dmO2aX;uJIF{e2G7 NE\zRYQzOCEQvF2= NVmyUndwWFhvNEe4JIlvcGmkaYTl[EBvd3Kvb4jpZ{BidmRiaInwc5hq[S2rbnT1Z4VlKEiLRj2x{tEh\XiycnXzd4lwdiCjczD3[YxtKGG|IFPPXE0zKGGwZDDQSE1NOSCneIDy[ZN{cW:w NELw[4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEW2NFA3Pyd-Mki1OlAxPjd:L3G+
EC109 NV3LdJhrTnWwY4Tpc44h[XO|YYm= NGHZeW4zOCEQvF2= M2LxW3BZNTR5ODDpcohq[mm2ZXSgco9zdW:6aXOgZY5lKGi7cH;4bYEucW6mdXPl[EBJUUZvMd8xJIV5eHKnc4Ppc44h[XNid3XscEBieyCFT2itNkBidmRiUFStUFEh\XiycnXzd4lwdg>? NWj3SIpWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OlAxPjdpPkK4OVYxODZ5PD;hQi=>
Tca8113 NWX0OGNETnWwY4Tpc44h[XO|YYm= M2Hab|AtKDVuIHHu[EAzPeLCid88US=> M{mxdVI1KGh? NEPMUo5z\WS3Y3XzJINmdGy3bHHyJIF2fG:yaHHnfS=> NX6xUoRoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[2OFA{OTZpPkK2OlQxOzF4PD;hQi=>
PDAC cell lines NXqweYNKTnWwY4Tpc44h[XO|YYm= NHnmVIczPSEQvF2= M3rOd|I1KGh? NHHCdo9qdmS3Y3XkJIEhfHKjboPsc4NifGmxbjDv[kBJVUeEMTDmdo9uKHSqZTDueYNt\XW|IITvJJRp\SCleYTvdIxie21? MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTV2NEe3NEc,OjV3NES3O|A9N2F-
PC3 M4\CemZ2dmO2aX;uJIF{e2G7 MnzSNlAhcHJ? Ml7nTWM2OCCob4KgTGlHNTIQsTDpcohq[mm2aX;uJIZweiCSQ{OgZ4VtdHNidX7k[ZIhdm:{bX;4bYMh[2:wZHn0bY9vKHejczCyNE0zPSEQvH3vcE9N MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd{OUG5Nkc,OTh5MkmxPVI9N2F-
DU 145 MV3GeY5kfGmxbjDhd5NigQ>? M2HxVVIxKGi{ MkjzTWM2OCCob4KgTGlHNTIQsTDpcohq[mm2aX;uJIZweiC2aHWgSHUhOTR3IHPlcIx{KHejczD+OFAuPTBizsztc4wwVA>? NUfMcYRnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi3NlkyQTJpPkG4O|I6OTl{PD;hQi=>
MCF7 M{jjPGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEPxRmw4OiCqcoO= M3vaR2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTVPGO{Bk\WyuczDh[pRmeiB5MjDodpMhfW6mZYKgbJlxd3irYzDjc45lcXSrb36gZpkhVVSWIHHzd4F6NCCLQ{WwJF0hOTlwNzFOwG0v NYnHUYNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkiyNFkzPTdpPkK4NlA6OjV5PD;hQi=>
MCF7 MV\GeY5kfGmxbjDhd5NigQ>? MYOyOEBpenN? MYXJcohq[mm2aX;uJI9nKEiLRj2xZYxxcGFiKIXub45wf25ib4Lp[4lvMSC2cnHud4NzcXC2aX;uZYwh[WO2aY\peJkh\XiycnXzd4VlKGmwIHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhOjRiaILzJJVv\GW{IHj5dI95cWNiY3;u[Il1cW:wIHL5JGhTTSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYpCpEwhUUN3MDC9JFIxNjJizszNMi=> NEL2VFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEKwPVI2Pyd-MkiyNFkzPTd:L3G+
MDA-MB-468 NED2XopCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M{HTZVczKGi{cx?= Mmj2RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPRFGtUWIuPDZ6IHPlcIx{KGGodHXyJFczKGi{czD1coRmeiCqeYDvfIlkKGOxbnTpeIlwdiCkeTDNWHQh[XO|YYmsJGlEPTBiPTC0OU4yKM7:TT6= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJyOUK1O{c,Ojh{MEmyOVc9N2F-
Assay
Methods Test Index PMID
Western blot HIF-1α ; VEGF / Angiopoietin 1 ; E-cadherin / N-cadherin / Vimentin ; HIF-1α ; VEGF / Angiopoietin 1 ; E-cadherin / N-cadherin / Vimentin 18729192 28052321 28560067
Growth inhibition assay Cell viability ; Cell viability 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 (from reference)

Animal Research:[1]
  • 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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 394.12
Formula

C13H20Cl4N2O3

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)

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Molarity Calculator

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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 2022-08-01)

Tech Support

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