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 50 publications

Purity & Quality Control

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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 NFjnZm1HfW6ldHnvckBie3OjeR?= NUC0WJV4OTEkgJpOwG0> Mk\CNlQhcA>? Mkjvd5VxeHKnc4OgTGlHNTIQsTDlfJBz\XO|aX;u MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODR5OUOzOkc,OzB2N{mzN|Y9N2F-
H460 MlOzSpVv[3Srb36gZZN{[Xl? NGrHbFUyOOLCid88US=> NUjM[XkzemWmdXPl[EBodHWlb4PlJJVxfGGtZTDhcoQhdGGldHH0[UBxem:mdXP0bY9vKHKjdHW= NXfkT|BKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CxNlgxOzVpPkOwNVI5ODN3PD;hQi=>
A549 M3XMO2Z2dmO2aX;uJIF{e2G7 M3zWUlEx6oDLzszN MnzBdoVlfWOnZDDncJVkd3OnIIXweIFs\SCjbnSgcIFkfGG2ZTDwdo9lfWO2aX;uJJJifGV? NGjFV|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEGyPFA{PSd-M{CxNlgxOzV:L3G+
SMMC7721 NF;VR3BHfW6ldHnvckBie3OjeR?= MUiyOUDPxE1? MmrVNlQhcA>? M{HmcolvcGmkaYTzJI1q\3KjdHnvckBw\iCVTV3DO|czOQ>? NGP2[oo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUS5OVM5OCd-Mkm0PVU{QDB:L3G+
EC9706 M13pOGZ2dmO2aX;uJIF{e2G7 M4HrN|IxKM7:TR?= MVvQXE01PzhiaX7obYJqfGWmIH7vdo1wgGmlIHHu[EBpgXCxeHnhMYlv\HWlZXSgTGlHNTIQsTDlfJBz\XO|aX;uJIF{KHenbHygZZMhS0:[LUKgZY5lKFCGLVyxJIV5eHKnc4Ppc44> NVnBPWFYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OlAxPjdpPkK4OVYxODZ5PD;hQi=>
EC109 MljRSpVv[3Srb36gZZN{[Xl? NUfVcnA3OjBizszN NXHYb3UyWFhvNEe4JIlvcGmkaYTl[EBvd3Kvb4jpZ{BidmRiaInwc5hq[S2rbnT1Z4VlKEiLRj2x{tEh\XiycnXzd4lwdiCjczD3[YxtKGG|IFPPXE0zKGGwZDDQSE1NOSCneIDy[ZN{cW:w MoC2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NkCwOlcoRjJ6NU[wNFY4RC:jPh?=
Tca8113 M4\zfGZ2dmO2aX;uJIF{e2G7 NFnJOXAxNCB3LDDhcoQhOjYkgJpOwG0> NGHxOFIzPCCq NV3qcVBEemWmdXPld{Bk\WyudXzhdkBifXSxcHjh[5k> M1XNXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NkSwN|E3Lz5{Nk[0NFMyPjxxYU6=
PDAC cell lines MmLGSpVv[3Srb36gZZN{[Xl? MmjYNlUh|ryP NGm2epMzPCCq NGK5OFRqdmS3Y3XkJIEhfHKjboPsc4NifGmxbjDv[kBJVUeEMTDmdo9uKHSqZTDueYNt\XW|IITvJJRp\SCleYTvdIxie21? NIq5c5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUW0OFc4OCd-MkW1OFQ4PzB:L3G+
PC3 NHzINnJHfW6ldHnvckBie3OjeR?= M1fUdFIxKGi{ NH7vVHdKSzVyIH\vdkBJUUZvMd8xJIlvcGmkaYTpc44h\m:{IGDDN{Bk\WyuczD1coRmeiCwb4Ltc5hq[yClb37kbZRqd25id3HzJFIxNTJ3IN88cY9tN0x? MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd{OUG5Nkc,OTh5MkmxPVI9N2F-
DU 145 MmHPSpVv[3Srb36gZZN{[Xl? NEO1N3YzOCCqch?= NVHabXJiUUN3MDDmc5IhUEmILUJOtUBqdmirYnn0bY9vKG[xcjD0bIUhTFViMUS1JINmdGy|IIfhd{B,PDBvNUCg{txud2xxTB?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDd{OUG5Nkc,OTh5MkmxPVI9N2F-
MCF7 MmC4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MknwO|IhcHK| MoXYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDd{IHjyd{B2dmSncjDofZBwgGmlIHPvcoRqfGmxbjDifUBOXFRiYYPzZZktKEmFNUCgQUAyQS55IN88UU4> MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDJyOUK1O{c,Ojh{MEmyOVc9N2F-
MCF7 NEGy[VNHfW6ldHnvckBie3OjeR?= MYCyOEBpenN? MkHOTY5pcWKrdHnvckBw\iCKSV[tNYFteGijIDj1cotvd3ewIH;ybYdqdilidILhcpNkemmydHnvcoFtKGGldHn2bZR6KGW6cILld5Nm\CCrbjDoeY1idiCPQ1[3JINmdGy|IHHmeIVzKDJ2IHjyd{B2dmSncjDofZBwgGmlIHPvcoRqfGmxbjDifUBJWkVibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5xsAtKEmFNUCgQUAzOC5{IN88UU4> Ml\vQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh{MEmyOVcoRjJ6MkC5NlU4RC:jPh?=
MDA-MB-468 NH25fVRCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mkj4O|IhcHK| MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2GQT3NRk01PjhiY3XscJMh[W[2ZYKgO|IhcHK|IIXu[IVzKGi7cH;4bYMh[2:wZHn0bY9vKGK7IF3UWEBie3OjeTygTWM2OCB;IES1MlEh|ryPLh?= M4XwZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MkC5NlU4Lz5{OEKwPVI2PzxxYU6=
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.
  • (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 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)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

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
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

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