Fludarabine

For research use only.

Catalog No.S1491 Synonyms: FaraA, Fludarabinum

71 publications

Fludarabine Chemical Structure

Molecular Weight(MW): 285.23

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 71 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  NIWwe|BHfW6ldHnvckBCe3OjeR?= NIHNUWQzOCEQvF2= NUPIS41xOjRiaB?= NWLQZ2ZycW6qaXLpeJMh\XiycnXzd4lwdiCxZjDJSG8> MUGyOVk1ODdzMh?=
MV-4-11 MX7BdI9xfG:|aYOgRZN{[Xl? MXqyMlUh|ryP NGez[lM1QCCq MnjlbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= Mn3lNlUyOTF3OEO=
THP-1 MlPNRZBweHSxc3nzJGF{e2G7 MV2yMlUh|ryP NGrIelU1QCCq NYrwWmlpcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> M1PYclI2OTFzNUiz
MOLM 13 Moj3RZBweHSxc3nzJGF{e2G7 MmLqNk42KM7:TR?= NFX0U2Q1QCCq MkLhbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NXjReolvOjVzMUG1PFM>
KBM3/Bu2506 NYfLdo8zSXCxcITvd4l{KEG|c3H5 NFv5cYUzNjVizszN M3T6NlQ5KGh? MorSbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MmTGNlUyOTF3OEO=
Nalm-6 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml62TWM2OD1zODFOwG0> MWSyOVA3OTFyMR?=
Reh NVX2fHNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HhemlEPTB;M{Cg{txO M{nEVFI2ODZzMUCx
U2937 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXHMeZhJUUN3ME2xOkDPxE1? MkfYNlUxPjFzMEG=
Mec-1 MlrLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1np[2lEPTExvK61NFAh|ryP NWnSbVR6OjVyNkGxNFE>
RPMI-8226 M2TIZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVKzcVN3UUN3ME21NFAh|ryP NYWyS2p{OjVyNkGxNFE>
Molt-4 NEDyfI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoX6TWM2OD1zOECg{txO Mlz1NlUxPjFzMEG=
Nalm-6-FluR NWnzbFBiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnS5TWM2OD1{NUCg{txO M{jNUVI2ODZzMUCx
Raji  M3jWVGZ2dmO2aX;uJGF{e2G7 NIL3SYQ{yqEQvF2= MoXqNlQwPDhxN{KgbC=> M3XrOolv\HWlZYOgZYNkfW23bHH0bY9veyCxZjDwOVMtKHB4MzDhcoQheDd|wrC= NGLMXnIzPDl2ME[5OS=>
PBMC M2LqNWZ2dmO2aX;uJGF{e2G7 M3qyO|UxNzFyMDFOwG0> MmqwNlQhcA>? NG\ad|RFVVOR M3fkSolvcGmkaYTzJHNVSVRzIIDoc5NxcG:{eXzheIlwdg>? MYOyOFkyOTh5Mh?=
MDA-231 MkXmSpVv[3Srb36gRZN{[Xl? MWqxNFAh|ryP Mnr1NlQhcA>? NVixdottTE2VTx?= MUTk[YNz\WG|ZYOgTWRQKGW6cILld5Nqd25? NGnOdXczPDlzMUi3Ni=>
624.38mel  NGrtcpVHfW6ldHnvckBCe3OjeR?= MkDsOVAh|ryP MnjFNlQhcA>? Mnz0SG1UVw>? NUDGU5dZ\GWlcnXhd4V{KEmGTzDlfJBz\XO|aX;u M1zTc|I1QTFzOEey
MDA-231 MXfGeY5kfGmxbjDBd5NigQ>? NHXyTlQ2OC1{MECg{txO NE\te5MzPCCq MV;EUXNQ NWPTOZdCcW6qaXLpeJMhUUSRIHHjeIl3cXS7IHnu[IVx\W6mZX70cJkhd2ZibWLORUBt\X[nbIO= NHrtUoIzPDlzMUi3Ni=>
624.38mel  MWfGeY5kfGmxbjDBd5NigQ>? NGC4Rms2OC1{MECg{txO MYGyOEBp MmLmSG1UVw>? NYfoRnZncW6qaXLpeJMhUUSRIHHjeIl3cXS7IHnu[IVx\W6mZX70cJkhd2ZibWLORUBt\X[nbIO= M1fVVlI1QTFzOEey
HMECs M2G2OmZ2dmO2aX;uJGF{e2G7 M2HqeFExOMLizszNxsA> NGjDdIM{PsLiaB?= NUXJSFRVcW6qaXLpeJMhUU[QzsRCpIFv\CCOUGOgbY5lfWOnZDDTWGFVOSCyaH;zdIhwenmuYYTpc44h[W6mIFnSSlEh\XiycnXzd4lwdg>? MVeyOFIyOTN{Nx?=
HMECs  M3yyTGZ2dmO2aX;uJGF{e2G7 MUexNFDDqM7:TdMg NEC0RVk{PsLiaB?= MlrsbY5pcWKrdIOgTWZP|rIEoH3l[IlifGWmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNuIHL1eEBvd3Rib3[gV3RCXDJ? NUPROmdDOjR{MUGzNlc>
BJAB MWnBdI9xfG:|aYOgRZN{[Xl? NInCT4o2yqEQvF2= NFnSZoIzPCCq M2XjZolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NHq2cGgzPDB3N{G0Oy=>
I-83 MUHBdI9xfG:|aYOgRZN{[Xl? M1\aflXDqM7:TR?= M{DRWFI1KGh? MofQbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? MnS0NlQxPTdzNEe=
NALM6 NWrsWlF1SXCxcITvd4l{KEG|c3H5 NV7Jd|hSPcLizszN MY[yOEBp M3zyZ4lv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MW[yOFA2PzF2Nx?=
DU-145 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFj6VVQxNTFyIN88[{9udA>? Mmm1OFghcMLi NVX5NnB3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? NI\QUJkzOzd|NEixOS=>
Nalm-6 MXnGeY5kfGmxbjDBd5NigQ>? MmO2NVDDqM7:TR?= M361[FEwOi92IHi= NXXFRVBZcW6mdXPld{BifXSxcHjh[5k> MUWyN|Y5OTJ{Mx?=
Reh NITET2RHfW6ldHnvckBCe3OjeR?= M3;IVVExyqEQvF2= NHvFW|gyNzJxNDDo NVjKZpZwcW6mdXPld{BifXSxcHjh[5k> MYGyN|Y5OTJ{Mx?=
Nalm-6 NUTLbJdrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoX4TWM2OCEkiMyxNQKBkc7:TR?= MUGyN|Y5OTJ{Mx?=
Reh MkTNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4ixfWlEPTBi4pk8NVDjiIoQvF2= M1\EPVI{PjhzMkKz
HEC1A MmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[xNFAuPTByIN88US=> NHTSfW8zPCCq MUXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MlnMNlM2QTV4OUe=
AN3CA NG\Ld29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWj4TYljOTByLUWwNEDPxE1? NFTuPGUzPCCq MXnpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mmn6NlM2QTV4OUe=
HEC50B M2GwUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vNSFExOC13MECg{txO M13VNFI1KGh? MUHpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> M3XCcFI{PTl3Nkm3
HEC1A M1LRdGFxd3C2b4Ppd{BCe3OjeR?= M4XXdVIxNzFyMDFOwG0> MYOyOEBp MXzpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= MmriNlM2QTV4OUe=
AN3CA MVvBdI9xfG:|aYOgRZN{[Xl? NIrVdJUzOC9zMECg{txO MV[yOEBp MmnabY5lfWOnczDhdI9xfG:|aYOgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= NIHIRoIzOzV7NU[5Oy=>
HEC50B NYHlZYRbSXCxcITvd4l{KEG|c3H5 MVWyNE8yODBizszN M1vnbFI1KGh? MVzpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NXuwVIZ7OjN3OUW2PVc>
EHEB Ml3FRZBweHSxc3nzJGF{e2G7 NIXUTVY1OCEQvF2= M4O4OlI1KGh? M1fkZYlv\HWlZYOgZZBweHSxc3nz MonZNlM1QTdyN{W=
A549 Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrXWIhKSzVyPUG1MlfDuTJwODFCuW0> MnHpNlM{PzdzOUK=
A549 GAPDH-deficient MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnriTWM2OD1zOD61xtEzNjNiwsXN Mo\WNlM{PzdzOUK=
CLL  MUPBdI9xfG:|aYOgRZN{[Xl? NWTpfHl5OTBizszNxsA> M4LOUFI1NTl4IHi= MWHpcoR2[2W|IHHwc5B1d3SrYzDj[YxtKGSnYYTo NHzwTnQzOjJyN{[4Oi=>
MEC1 NYDOV3A1SXCxcITvd4l{KEG|c3H5 MV2xNFDDqM7:TR?= NGO3RWo4OiCq MoH6bY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgQ>? MX[yNlE{Ojl5Mx?=
U937  NFrBb4lCeG:ydH;zbZMhSXO|YYm= MkTkNE45KM7:TR?= NUf3TmNEPC12ODDo MV7pcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NGm5epUzOjB5NEewNC=>
U937  M2r4dGFxd3C2b4Ppd{BCe3OjeR?= Mm[3NUDPxE1? NHXBTIk6PiCq MXvpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= MmnLNlIxOjN3MkO=
Daudi NF7vXFdCeG:ydH;zbZMhSXO|YYm= MkDjNlAh|ryP NFPYN5I6PiCq Ml\SbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MmPONlIxOjN3MkO=
J45.01 NXL2[YZ4SXCxcITvd4l{KEG|c3H5 MmTLNUDPxE1? NEH3UXo6PiCq MX;pcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NHvOcYMzOjB{M{WyNy=>
RPMI 8226 NHfReVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NU\1bFJMUUN3ME2yOU46yqEEsdMgN{44KM7:TR?= NHrwdWszOTl2OEK2OC=>
CEM NWC1N2VnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{nWVmlEPTB;Mj60xsDDucLiMD60JO69VQ>? NIDseYMzOTl2OEK2OC=>
Raji M1SzR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPyTWM2OD1yLkS3xsDDucLiMD6wOEDPxE1? M4TxeFIyQTR6Mk[0
U937 NELoR2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTBwMkVCpOKyyqByLkC0JO69VQ>? NFviO2ozOTl2OEK2OC=>
K562 M3fremdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXxbYF1UUN3ME2wMlQ1yqEEsdMgNE4xPSEQvF2= MV[yNVk1QDJ4NB?=
NALM-6 M4jucGFxd3C2b4Ppd{BCe3OjeR?= NWHLbnFSOTBizszNxsA> MYWyOEBp NEjBb5NqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPsbYdpfGy7 NWLud2g6OjF4OUmzPFM>
JMV-3 MWXBdI9xfG:|aYOgRZN{[Xl? NFXqUJAyOCEQvF5CpC=> MXiyOEBp Mm\kbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|bHnnbJRtgQ>? MlXpNlE3QTl|OEO=
EHEB MVzGeY5kfGmxbjDBd5NigQ>? MWq1MVUxKM7:TR?= M164N|I1KGh? MVnk[YNz\WG|ZYOgdFIyKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> NW[5eVNQOjFzNkizPVE>
JVM-2  NHvzXYFHfW6ldHnvckBCe3OjeR?= M1HGSVMxKM7:TR?= NV23WnB3OjRiaB?= NFy1[YVl\WO{ZXHz[ZMheDJzIHX4dJJme3Orb36= MWKyNVE3QDN7MR?=
KBM3/Bu2506 NWrFUphlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PORWlEOjB;MD62O{DDvU1? M4PUblIxQTN|NUC5
KBM3/Bu2506 M{jG[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWwNE43KM7:TR?= M4LPblI1KGh? NF:zUpFqdmO{ZXHz[ZMhfGinIHPlcIwh\nKjY4Tpc44hcW5iUz3wbIF{\Q>? M3uwXVIxQTN|NUC5
MDA-MB-231 M3PZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jubmlEPTB;ND6wJO69VQ>? Moj5NlA1PDd|OUC=
MCF-7 NEX2OYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe0PYpKSzVyPUG1MlAh|ryP NHnSdVczODR2N{O5NC=>
HLE-B3  NVrBbXJNTnWwY4Tpc44hSXO|YYm= NV\GVlJYOjVizszN MVy0PEBp NVXXR|B7[myxY3vzJGlHVi4Qs,MAl4lv\HWlZXSgV3RCXDFicHjvd5Bpd3K7bHH0bY9vKGGwZDDJSG8h\XiycnXzd4lwdg>? MlTDNlA1OzVzNUi=
K562 MmLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPFRpZbPzJiaB?= M4DxeWlEPTB;Mz6zJI5O NH[yW2MzODNyN{G5PC=>
BW-225 NHfiNI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LjcWlEOjB;MT6zO{DEnzFy4pkSPOKh|ryPwrC= M3fBTFE5PjZzM{iw
OH-65 NIrvUJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3jOYhXUUN{ME2xMlM4KMPZMUFijLI5yqEQvF5CpC=> NWLFXGNROTh4NkGzPFA>
GR-145 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGOyd|hKSzJyPUKuO|Qhy5diMUFijLI5KCEQvF5CpC=> NYHnUIF5OTh4NkGzPFA>
A549 NHnyPFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXj[4hKSzJyPUWuOFghy5diMUFijLI5KM7:TdMg MlrsNVg3PjF|OEC=
CaSki  NVTqfJZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|IxRTFwM{egx7chOTEkiKK3JO69VcLi Mn7QNVg3PjF|OEC=
ZMK-1 M1fCN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|IxRTFwM{egx7chOTEkiKK2JO69VcLi MkXtNVg3PjF|OEC=
SKW6.4 M4\XT2Fxd3C2b4Ppd{BCe3OjeR?= NF34bI0xNjBzLUGwJO69VQ>? MlmwNlQwPDhiaB?= M3PYeolv\HWlZYOgZ4VtdCCmZXH0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLTDk[ZBmdmSnboSgcYFvdmW{ NH3aVnoyQDB7MkO0NC=>
RPMI 8226 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnHeYkzPCCq NIDLNI5KSzVyPUGuOVTDqM7:TR?= MX[xO|k4PjF6Nh?=
MM.1S NH\iPW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3hOYY1QCCq MUPJR|UxRTF|LkS4xsDPxE1? NULsRmM3OTd7N{[xPFY>
MM.1R NVzVbpBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTyeI1xPDhiaB?= NY\reVZZUUN3ME2zN{44QSEQvF2= NHHqfZYyPzl5NkG4Oi=>
U937 Ml7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPYTWM2OD1|LEKwNEDDuSB3NkCgcm0> NHqxR|cyPTl|MEO2NS=>

... 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