An orally bioavailable iron chelator with anticancer activity; selective for (Fe(III) over Cu(II)

Deferasirox – 25 mg

Brand:
Cayman
CAS:
201530-41-8
Storage:
-20
UN-No:
Non-Hazardous - /

Deferasirox is an orally bioavailable synthetic, tridentate iron chelator that binds iron at a 2:1 ratio.{36858} It is selective for iron (Fe(III)) over Cu(II), Zn(II), Mg(II), and Ca(II) but does bind to Al(III). Deferasirox decreases iron levels in iron-loaded rat heart cells in vitro by 45.8 and 55.6% compared to control levels when used at concentrations of 160 and 320 µM, respectively.{27434} In hypertransfused rats, deferasirox (200 mg/kg) decreases radiolabeled liver iron levels from 41 to 21.7% and blood iron levels from 8.2 to 3.4%.{27434} It is primarily excreted via the fecal route, in contrast to the iron chelator deferoxamine (Item No. 14595).{27434} Deferasirox also inhibits proliferation of SAS human oral squamous carcinoma cells (EC50 = 21 µM), decreases cyclin D1 protein levels, and increases protein levels of N-Myc downregulated gene 1 (NDRG1) and NDRG3.{38960} It acts in a synergistic manner when used in combination with gemcitabine (Item Nos. 11690 | 9003096) to reduce proliferation of BxPC-3 pancreatic cancer cells in vitro and reduce tumor growth in a BxPC-3 mouse xenograft model when administered at a dose of 200 mg/kg.{36859} Formulations containing deferasirox have been used in the treatment of β-thalassemia and chronic iron overload.  

 

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An orally bioavailable iron chelator with anticancer activity; selective for (Fe(III) over Cu(II), Zn(II), Mg(II), and Ca(II) but does bind to Al(III); decreases iron levels in iron-loaded rat heart cells in vitro by 45.8 and 55.6% compared to control levels at 160 and 320 µM; decreases radiolabeled liver iron levels from 41 to 21.7% and blood iron levels from 8.2 to 3.4% in hypertransfused rats at 200 mg/kg; inhibits proliferation of SAS human oral squamous carcinoma cells (EC50 = 21 µM); act synergistically with gemcitabine in vitro to inhibit proliferation and in vivo to reduce tumor growth at 200 mg/kg in a BxPC-3 mouse xenograft model

Formal name: 4-[3,5-bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl]-benzoic acid

Synonyms:  ICL670A

Molecular weight: 373.4

CAS: 201530-41-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Metal Chelators||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Ferroptosis||Research Area|Cardiovascular System|Blood|Erythrocytes & Hemoglobin||Research Area|Cell Biology|Cell Death|Ferroptosis

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