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Fludarabine

For research use only.

Catalog No.S1491 Synonyms: FaraA, Fludarabinum

94 publications

Fludarabine Chemical Structure

CAS No. 21679-14-1

Fludarabine (FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.

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Selleck's Fludarabine has been cited by 94 publications

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Choose Selective STAT Inhibitors

Biological Activity

Description Fludarabine (FaraA, Fludarabinum) is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.
Targets
STAT1 [4]
(Vascular smooth muscle cells)
In vitro

Fludarabine efficiently inhibits the proliferation of RPMI 8226 cells with IC50 of 1.54 μg/mL. The IC50 of Fludarabine against MM.1S and MM.1R cells is 13.48 μg/mL and 33.79 μg/mL, respectively. In contrast, U266 cells are resistant to Fludarabine with IC50 of 222.2 μg/mL. Fludarabine treatment results in increased number of cells in the G1 phase of cell cycle, accompanied with a concomitant reduction of cells at the S phase of cell cycle in a time-dependent manner. Fludarabine induces a cell cycle block and triggers apoptosis in MM cells. Fludarabine triggers time-dependent cleavage of caspase-8, -9, and -3, -7, followed by PARP cleavage. Fludarabine increases expression of Bax in a time-dependent fashion, while the expression of Bak doesn't change. After exposure to Fludarabine for 12 hours, RPMI 8226 cells shows a loss of membrane potential with 61.05% of the cells expressing low fluorescence of rhodamine 123 compared with 8.62% of cells in untreated control. [1] To enhance solubility, Fludarabine is formulated as the monophosphate (F-ara-AMP, fudarabine), which is instantaneously and quantitatively dephosphorylated to the parent nucleoside upon intravenous infusion. Inside the cells rephosphorylation occurs which leads to fuoroadenine arabinoside triphosphate (F-ara-ATP), the major cytotoxic metabolite of F-ara-A. [2] Fludarabine can also induce pro-inflammatory stimulation of monocytic cells, as evaluated by increased expression of ICAM-1 and IL-8 release. [3] Fludarabine does not affect the growth of ovarian cancer cell lines, whereas it induces marked and dose-dependent inhibition of proliferation in melanoma cell lines. [4] Fludarabine induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Interestingly, Fludarabine does not significantly affect the phosphorylation of these three STAT proteins. Fludarabine (1.5 mg) significantly prevents STAT-1 phosphorylation and also reduces the increased amount of this protein. No significant changes are demonstrated in JAK2 phosphorylation at 2 days, but Fludarabine inhibits JAK2-increased expression at 7 days. Fludarabine specifically inhibits STAT-1 activation without affecting other STAT proteins and consequently diminishes VSMC proliferation. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jeko-1  NIXHXGFHfW6ldHnvckBCe3OjeR?= M2rFT|IxKM7:TR?= MkT0NlQhcA>? NWWxXINtcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDJSG8> NVi4V3lORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OFA4OTJpPkK1PVQxPzF{PD;hQi=>
MV-4-11 NUTxb3B4SXCxcITvd4l{KEG|c3H5 M2TlUFIvPSEQvF2= MY[0PEBp Mlq0bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MlfXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUG1PFMoRjJ3MUGxOVg{RC:jPh?=
THP-1 MYXBdI9xfG:|aYOgRZN{[Xl? NF7iOHgzNjVizszN NU\seWFzPDhiaB?= M{HiOIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NFOxXnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUGxNVU5Oyd-MkWxNVE2QDN:L3G+
MOLM 13 MYHBdI9xfG:|aYOgRZN{[Xl? MnjMNk42KM7:TR?= NFXtXYg1QCCq MYfpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTFzMUW4N{c,OjVzMUG1PFM9N2F-
KBM3/Bu2506 NHPuXIJCeG:ydH;zbZMhSXO|YYm= MXyyMlUh|ryP NWrBNnc3PDhiaB?= M4n5bolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MnezQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVzMUG1PFMoRjJ3MUGxOVg{RC:jPh?=
Nalm-6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXRTWM2OD1zODFOwG0> NVH0TIVMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlEyODFpPkK1NFYyOTBzPD;hQi=>
Reh NF\oSpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfnTHpKSzVyPUOwJO69VQ>? MoDYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkGxNFEoRjJ3ME[xNVAyRC:jPh?=
U2937 Mn;qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvtbmxGUUN3ME2xOkDPxE1? NWPLS4c6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWwOlEyODFpPkK1NFYyOTBzPD;hQi=>
Mec-1 NX7hendDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHnOO2VKSzVy78{eOVAxKM7:TR?= MkPoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkGxNFEoRjJ3ME[xNVAyRC:jPh?=
RPMI-8226 NEHKeldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37hO2lEPTB;NUCwJO69VQ>? M1[1XlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3ME[xNVAyLz5{NUC2NVExOTxxYU6=
Molt-4 NFfHWlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\UNmVKSzVyPUG4NEDPxE1? MnLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjVyNkGxNFEoRjJ3ME[xNVAyRC:jPh?=
Nalm-6-FluR NEfXfVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\NdZBKSzVyPUK1NEDPxE1? MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTB4MUGwNUc,OjVyNkGxNFE9N2F-
Raji  MUPGeY5kfGmxbjDBd5NigQ>? NIDOdow{yqEQvF2= NUfMe29xOjRxNEivO|IhcA>? MXzpcoR2[2W|IHHjZ5VufWyjdHnvcpMhd2ZicEWzMEBxPjNiYX7kJJA4O8Li MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl2ME[5OUc,OjR7NEC2PVU9N2F-
PBMC NHizdlJHfW6ldHnvckBCe3OjeR?= M1i1c|UxNzFyMDFOwG0> MX[yOEBp MkHUSG1UVw>? MXnpcohq[mm2czDTWGFVOSCyaH;zdIhwenmuYYTpc44> NE\1em89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxNVg4Oid-MkS5NVE5PzJ:L3G+
MDA-231 Mk\HSpVv[3Srb36gRZN{[Xl? MU[xNFAh|ryP MXOyOEBp NXvUZ2t{TE2VTx?= NWO0PIQ2\GWlcnXhd4V{KEmGTzDlfJBz\XO|aX;u MnfpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUG4O|IoRjJ2OUGxPFczRC:jPh?=
624.38mel  MnnwSpVv[3Srb36gRZN{[Xl? MXS1NEDPxE1? NH\mUmQzPCCq M3i5fmROW09? MWHk[YNz\WG|ZYOgTWRQKGW6cILld5Nqd25? Ml7LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MUG4O|IoRjJ2OUGxPFczRC:jPh?=
MDA-231 MnvxSpVv[3Srb36gRZN{[Xl? M1G5WVUxNTJyMDFOwG0> NF70RmozPCCq MV;EUXNQ NEHGcllqdmirYnn0d{BKTE9iYXP0bZZqfHliaX7k[ZBmdmSnboTsfUBw\iCvUl7BJIxmfmWucx?= NILZ[ng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmxNVg4Oid-MkS5NVE5PzJ:L3G+
624.38mel  MmPlSpVv[3Srb36gRZN{[Xl? M4iySlUxNTJyMDFOwG0> MWqyOEBp M2PDPWROW09? M37LdIlvcGmkaYTzJGlFVyCjY4Tpeol1gSCrbnTldIVv\GWwdHz5JI9nKG2UTlGgcIV3\Wy| M1[xOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUGxPFczLz5{NEmxNVg4OjxxYU6=
HMECs NX\Qe4JCTnWwY4Tpc44hSXO|YYm= NGDN[WYyODEEoN88UeKh NXT5VYVROzcEoHi= NIPhUoZqdmirYnn0d{BKTk8Qs9MgZY5lKEySUzDpcoR2[2WmIGPURXQyKHCqb4PwbI9zgWyjdHnvckBidmRiSWLGNUBmgHC{ZYPzbY9v NXi0dIlCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSyNVE{OjdpPkK0NlEyOzJ5PD;hQi=>
HMECs  NETQN2ZHfW6ldHnvckBCe3OjeR?= Ml3JNVAxyqEQvF5CpC=> NEm3dYU{PsLiaB?= MkD2bY5pcWKrdIOgTWZP|rIEoH3l[IlifGWmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNuIHL1eEBvd3Rib3[gV3RCXDJ? NEO5cYU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEKxNVMzPyd-MkSyNVE{Ojd:L3G+
BJAB MoTXRZBweHSxc3nzJGF{e2G7 NUjCU4VwPcLizszN NEfjXFAzPCCq MljWbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M2DtVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEW3NVQ4Lz5{NEC1O|E1PzxxYU6=
I-83 M3ftSmFxd3C2b4Ppd{BCe3OjeR?= NEXSV4w2yqEQvF2= M1LPeVI1KGh? NIjCZXVqdmS3Y3XzJINmdGxiYYDvdJRwe2m| MnLyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRyNUexOFcoRjJ2MEW3NVQ4RC:jPh?=
NALM6 NWq1VJNpSXCxcITvd4l{KEG|c3H5 NHPGfo82yqEQvF2= Mmi3NlQhcA>? M4T1cIlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? M1LPeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MEW3NVQ4Lz5{NEC1O|E1PzxxYU6=
DU-145 M17KOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWCyT|ZzOC1zMDFOwIcwdWx? MlzVOFghcMLi M2LlV4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz M2\PSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|N{O0PFE2Lz5{M{ezOFgyPTxxYU6=
Nalm-6 M4rqOWZ2dmO2aX;uJGF{e2G7 MlvmNVDDqM7:TR?= NE\jcJkyNzJxNDDo MWHpcoR2[2W|IHH1eI9xcGGpeR?= NF7pR2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4NVIzOyd-MkO2PFEzOjN:L3G+
Reh MV\GeY5kfGmxbjDBd5NigQ>? NVfwZ|dUOTEEoN88US=> MljJNU8zNzRiaB?= Ml;1bY5lfWOnczDheZRweGijZ4m= NEnSb3Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[4NVIzOyd-MkO2PFEzOjN:L3G+
Nalm-6 NX\XUoFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3ji[WlEPTBi4pk8NVDjiIoQvF2= NYLuTHp7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PFEzOjNpPkKzOlgyOjJ|PD;hQi=>
Reh NHfxcINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF;0PVlKSzVyIPMIwFEx6oDLzszN NWTjcZRvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2PFEzOjNpPkKzOlgyOjJ|PD;hQi=>
HEC1A NGjBR|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV6xNFAuPTByIN88US=> NXvT[GFzOjRiaB?= M{DY[IlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NGfOd4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W5OVY6Pyd-MkO1PVU3QTd:L3G+
AN3CA M3rGTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;UbFExOC13MECg{txO M4DFSFI1KGh? NYrPbGdFcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? MnP1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3OUW2PVcoRjJ|NUm1Olk4RC:jPh?=
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HEC1A MmTBRZBweHSxc3nzJGF{e2G7 MWCyNE8yODBizszN M4\xVlI1KGh? M2Dw[Ylv\HWlZYOgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy Mn3KQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN3OUW2PVcoRjJ|NUm1Olk4RC:jPh?=
AN3CA MoKxRZBweHSxc3nzJGF{e2G7 NWPHRVVJOjBxMUCwJO69VQ>? Ml;NNlQhcA>? MV7pcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzV7NU[5O{c,OjN3OUW2PVc9N2F-
HEC50B NGDNbZJCeG:ydH;zbZMhSXO|YYm= NVq1TYJzOjBxMUCwJO69VQ>? M4HVWlI1KGh? NGnST4FqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NH\1V4Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{W5OVY6Pyd-MkO1PVU3QTd:L3G+
EHEB NHHxPVBCeG:ydH;zbZMhSXO|YYm= MmSwOFAh|ryP Mlm0NlQhcA>? MkXmbY5lfWOnczDhdI9xfG:|aYO= NHKzPG09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{S5O|A4PSd-MkO0PVcxPzV:L3G+
A549 MljLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF3LkhCtVIvQCEEtV2= NHi4NWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{O3O|E6Oid-MkOzO|cyQTJ:L3G+
A549 GAPDH-deficient M4[zeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHTLSnRKSzVyPUG4MlXDuTJwMzFCuW0> MYO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN5N{G5Nkc,OjN|N{exPVI9N2F-
CLL  NX;K[Jc1SXCxcITvd4l{KEG|c3H5 M3T3UlExKM7:TdMg NXTad2lOOjRvOU[gbC=> MnrMbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> NV\J[IoyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKyNFc3QDZpPkKyNlA4Pjh4PD;hQi=>
MEC1 NIOwe4RCeG:ydH;zbZMhSXO|YYm= MWixNFDDqM7:TR?= M17jbVczKGh? NHO2PYpqdmS3Y3XzJIFxd3C2b4Ppd{B{cWewaX\pZ4FvfGy7 M3K3cVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MUOyPVc{Lz5{MkGzNlk4OzxxYU6=
U937  M13FVWFxd3C2b4Ppd{BCe3OjeR?= NEjX[poxNjhizszN NIrEfGc1NTR6IHi= MmP3bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NVi3RY17RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkKwO|Q4ODBpPkKyNFc1PzByPD;hQi=>
U937  MXHBdI9xfG:|aYOgRZN{[Xl? NXHTfVFjOSEQvF2= MV[5OkBp NVj5U5plcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> M2PwNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{MEKzOVI{Lz5{MkCyN|UzOzxxYU6=
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SJ-GBM2 MoTKdWhVWyCjc4PhfS=> NWLOb2I{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> MkHBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NFm3eGdyUFSVIHHzd4F6 MoK0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M4GyN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NYroN45veUiWUzDhd5NigQ>? MUDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= Mn\RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 M1fNfpFJXFNiYYPzZZk> Mn;PdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 M2rZdJFJXFNiYYPzZZk> NWO1N|BbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= NWnPVZVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 NEDWbphyUFSVIHHzd4F6 MVPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDORlE3PDNiY3XscJM> NYfXW4pkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MUjxTHRUKGG|c3H5 NY\sWIdweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NInrSWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SJ-GBM2 Ml7tdWhVWyCjc4PhfS=> NXTZ[XdneUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 MlrCdWhVWyCjc4PhfS=> MVzxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 NGm2TFFyUFSVIHHzd4F6 MV;xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFE5KGOnbHzz NX;DNJh1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 Mo\idWhVWyCjc4PhfS=> NYeyeHNJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| NYDaVohoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MXXxTHRUKGG|c3H5 M4\uXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KE:{dHjv[49v[WxiM1Sgeoli[mmuaYT5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD MVTxTHRUKGG|c3H5 NY\YUFNqeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiT4L0bI9od26jbDCzSEB3cWGkaXzpeJkhe2O{ZXXuJIZweiCURDDj[Yxtew>? NHnOO409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
procaspase-9 / procaspase-3; 

PubMed: 27223263     


Procaspase-9 and procaspase-3 were analyzed by Western blot in CLL cells from three patients after a 48 h-incubation in the absence or presence of 3 μM aphidicolin (APC) with or without fludarabine at 0.3 and 1 μM. β-Actin served as a loading control.

p-p53 / p53; 

PubMed: 27223263     


(A–B) CLL cells from 3 different patients were incubated for 24 h with fludarabine at the indicated concentrations in the absence or presence of 3 μM aphidicolin (APC). Phosphorylation of p53 at Ser-15 and total p53 were analyzed by Western blot. Data sho䲧疝Ỵ疞㧀疜膉痘 瘿�෋ᾰƌ෋à 㺣痖帉痖Ѐ瑖堘𢡄빢᎒෋à鑸᎒彿堙奋堙巫堙᎒ﻺ᎒彿堙ﻮ᎒

STAT1; 

PubMed: 26677135     


Representative western blot analysis of STAT1 in RAW 264.7 cells treated with STAT1 inhibitor fludarabine (Flu) for 24 h.

27223263 26677135
Immunofluorescence
α-SMA / Vimentin; 

PubMed: 28322315     


FLU (50 μM) reduces the expression of α-SMA and Vimentin protein in primary mouse activated HSCs (Hepatic Stellate Cells).

28322315
Growth inhibition assay
Cell viability ; 

PubMed: 24956101     


CLL cells RPMI/0.1% FBS were cultured on 0.5% BSA or 150 nM MMP-9 for 1 h prior to adding the indicated concentrations of fludarabine (Fluda). After 48 h (Fluda) cell viability was determined by flow cytometry using FITC-Annexin V and PI.

24956101
In vivo Tumors treated with PBS grow rapidly to approx-imately 10-fold their initial volume in 25 day, whereas, the tumors in the Fludarabine at 40 mg/kg increase less than 5-fold. A significant antitumor effect of 40 mg/kg Fludarabine on RPMI8226 tumor growth is demonstrated. RPMI8226 tumors treated with 40 mg/kg Fludarabine at day 10 increase apoptotic nuclei. Fludarabine is effective in suppressing RPMI8226 myeloma xenografts in SCID mice. [1]

Protocol

Cell Research:

[1]

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  • Cell lines: Dexamethasone-sensitive (MM.1S) and -resistant (MM.1R) human MM cell lines, RPMI8226 and U266 cell lines
  • Concentrations: 2 μg/mL
  • Incubation Time: 24 hours
  • Method:

    After treated with Fludarabine or control, dexamethasone-sensitive (MM.1S) and -resistant (MM.1R) human MM cell lines, RPMI8226 and U266 cell lines (5 × 105 cells) are washed twice in phosphate-buffered saline (PBS) and fixed with 70% ice-cold ethanol, then centrifuged and suspended in PBS containing 100 μg/mL RNase A. After incubated for 30 minutes at 37 ºC, samples are resuspended in 25 μg/mL propidium iodide. Flow cytometry is performed on a FACSCalibur automated system. Apoptosis is determined by Annexin V-FITC apoptosis detection kit, according to the manufacturer's instructions. For TUNEL (terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate nick end labeling) assay, cells are analyzed by flow cytometry using the in situ cell death detection kit.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Severe combined immunodeficient (SCID) mice bearing RPMI 8226 cells
  • Dosages: 40 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 57 mg/mL (199.83 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL (suspension)

* 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 285.23
Formula

C10H12FN5O4

CAS No. 21679-14-1
Storage powder
in solvent
Synonyms FaraA, Fludarabinum
Smiles C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)O)F)N

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04526795 Not yet recruiting Drug: Cytarabine|Drug: Fludarabine|Drug: Pegcrisantaspase Blast Phase Chronic Myelogenous Leukemia BCR-ABL1 Positive|Recurrent Acute Biphenotypic Leukemia|Recurrent Acute Lymphoblastic Leukemia|Recurrent Acute Myeloid Leukemia|Recurrent Chronic Myelogenous Leukemia BCR-ABL1 Positive|Recurrent T-Cell Prolymphocytic Leukemia|Refractory Acute Biphenotypic Leukemia|Refractory Acute Lymphoblastic Leukemia|Refractory Acute Myeloid Leukemia|Refractory Chronic Myelogenous Leukemia BCR-ABL1 Positive|Refractory T-Cell Prolymphocytic Leukemia M.D. Anderson Cancer Center|National Cancer Institute (NCI) December 31 2020 Phase 1
NCT03832127 Not yet recruiting Drug: 18F-Fludarabine Myeloma Nantes University Hospital|Cyceron April 1 2019 Phase 1

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

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 1:

    how to re-suspend and deliver the inhibitor for in vivo experiments?

  • Answer:

    For S1491, Fludarabine, we tested a vehicle: 30% Propylene glycol, 5% Tween 80, 65% D5W that you can resuspend the compound in at up to 30mg/ml. It's a suspension and can only be given via oral gavage.

STAT Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID