Deferasirox (ICL-670)

Catalog No.S1712 Synonyms: CGP-72670

For research use only.

Deferasirox (ICL-670, CGP-72670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.

Deferasirox (ICL-670) Chemical Structure

CAS No. 201530-41-8

Selleck's Deferasirox (ICL-670) has been cited by 11 Publications

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Biological Activity

Description Deferasirox (ICL-670, CGP-72670) is an iron chelator, also a cytochrome P450 3A4 inducer, Cytochrome P450 2C8 inhibitor, and Cytochrome P450 1A2 inhibitor. Deferasirox-induced iron depletion promotes BclxL downregulation and cell death.
In vitro

Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. [1] Deferasirox incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples. [2] Deferasirox inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. [3] Deferasirox is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MDA-MB-231 M4TOSGN6fG:2b4jpZ4l1gSCjc4PhfS=> NFnsNow6PiCqcoO= MV3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDl4IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PM7:TR?= NIfvW4U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MECwOVcxQCd-MkCwNFU4ODh:L3G+
MIAPaCa2 NWjjSm0yS3m2b4TvfIlkcXS7IHHzd4F6 M1;1bFk3KGi{cx?= MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA6PiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVEx|ryP MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODByNUewPEc,OjByMEW3NFg9N2F-
SK-N-MC NH60PJJVd3irY3n0fUBie3OjeR?= M1vVXHRwgGmlaYT5JIlvKGi3bXHuJHNMNU5vTVOgZ4VtdHNiYomgUXRVKG2ndHjv[EwhUUN3ME2yNE42PM7:TR?= MoTsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjByNEG2O|IoRjJyMESxOlczRC:jPh?=
Sf9 NYmxU3hKTnWwY4Tpc44h[XO|YYm= NEmw[HYzOCCvaX7z NF7rVHRKdmirYnn0bY9vKG:oIHj1cYFvKE2UUESgc5ZmemW6cILld5Nm\CCrbjDT[lkh[2WubDDt[Y1jemGwZTD2[ZNq[2ynczDhd5Nme3OnZDDhd{B2eHSja3Wgc4YhYzOKXT3ld5Rz[WSrb3ytNVdj\XSjLVSt[4x2[3W{b37p[IUhcW5icILld4Vv[2Vib3[gRXRRKGGwZDDHV2ghdWWjc4Xy[YQh[W[2ZYKgNlAhdWmwczDifUBu\W2kcnHu[UB3\XOrY3zlJJRz[W6|cH;yeEBie3OjeTygTWM2OD1|Nj61{txO NH7kSmg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{m1OlExOSd-MkO5OVYyODF:L3G+
SJ-GBM2 NILpXmlyUFSVIHHzd4F6 MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= Mo\0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 NFrwPGRyUFSVIHHzd4F6 M1jDVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NHLvTZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NGLqfpVyUFSVIHHzd4F6 NE\SW3hyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> MlflQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MWrxTHRUKGG|c3H5 M4XmUpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot CDK2 / CDK4 / CDK6 / Cyclin A / Cyclin B / Cyclin D1 / Cyclin E / p53 / p27 / p21 ; TFR1 / Ferroportin ; Pro-caspase-3 / Pro-caspase-8 / Pro-caspase-9 / BAX / NDRG1 / c-Myc / p-mTOR 26965928
Immunofluorescence Bax / TOM22 ; Cytochrome c 28139717
Growth inhibition assay Cell viability ; Cell viability 26965928 28139717
In vivo Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. Deferasirox treatment also enhances the host inflammatory response to mucormycosis. Deferasirox synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. [1] Deferasirox administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%.Deferasirox is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. Deferasirox is 99.2% bound to plasma proteins. [4] Deferasirox monotherapy modestly prolongs survival of mice with IPA. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5%Tween 80 +50 % H2O
For best results, use promptly after mixing.

3.7 mg/mL

Chemical Information

Molecular Weight 373.36
Formula

C21H15N3O4

CAS No. 201530-41-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C(=C1)C2=NN(C(=N2)C3=CC=CC=C3O)C4=CC=C(C=C4)C(=O)O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04423237 Active not recruiting Drug: Deferasirox Iron Overload University of Pisa|IRCCS Burlo Garofolo|University of Genova September 30 2020 --
NCT03920657 Unknown status Drug: Deferasirox Myelodysplastic Syndromes Fondazione Italiana Sindromi Mielodisplastiche-ETS July 2019 Phase 2
NCT03372083 Completed Drug: Deferasirox Iron Overload Novartis Pharmaceuticals|Novartis January 16 2018 Phase 4
NCT02663752 Terminated Procedure: Bone marrow aspirate|Drug: Deferasirox Myelodysplastic Syndrome Novartis Pharmaceuticals|Novartis May 30 2016 Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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Handling Instructions

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