Fludarabine

For research use only.

Catalog No.S1491 Synonyms: FaraA, Fludarabinum

82 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 82 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  MmnXSpVv[3Srb36gRZN{[Xl? Mk\QNlAh|ryP NETPZmUzPCCq NU\xSpRJcW6qaXLpeJMh\XiycnXzd4lwdiCxZjDJSG8> NFfNVpczPTl2MEexNi=>
MV-4-11 NGHM[4FCeG:ydH;zbZMhSXO|YYm= MUiyMlUh|ryP M4f6[lQ5KGh? M37iZ4lv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MXKyOVEyOTV6Mx?=
THP-1 Mki2RZBweHSxc3nzJGF{e2G7 MnW0Nk42KM7:TR?= Ml\4OFghcA>? Mme0bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= Mke3NlUyOTF3OEO=
MOLM 13 NELLW3lCeG:ydH;zbZMhSXO|YYm= MknQNk42KM7:TR?= NHfTcnc1QCCq Ml36bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NXzpcVE4OjVzMUG1PFM>
KBM3/Bu2506 MnfvRZBweHSxc3nzJGF{e2G7 M{HWUVIvPSEQvF2= M3nONVQ5KGh? M{HROolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 M3mwc|I2OTFzNUiz
Nalm-6 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkfvTWM2OD1zODFOwG0> NHn0O5MzPTB4MUGwNS=>
Reh MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFSyPGNKSzVyPUOwJO69VQ>? MmfUNlUxPjFzMEG=
U2937 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRTF4IN88US=> M3PHNFI2ODZzMUCx
Mec-1 NWS2PVNVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1ez[2lEPTExvK61NFAh|ryP NWHJeVdlOjVyNkGxNFE>
RPMI-8226 M4rlcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHub5ZuUUN3ME21NFAh|ryP MYWyOVA3OTFyMR?=
Molt-4 M4XN[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{f2dmlEPTB;MUiwJO69VQ>? MVOyOVA3OTFyMR?=
Nalm-6-FluR NVfE[WJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT6[|hKSzVyPUK1NEDPxE1? M2CyVlI2ODZzMUCx
Raji  M4\lOmZ2dmO2aX;uJGF{e2G7 MorNN:Kh|ryP M1y0fVI1NzR6L{eyJIg> NHHmOXhqdmS3Y3XzJIFk[3WvdXzheIlwdnNib3[gdFU{NCCyNkOgZY5lKHB5M9Mg NWPDSo5YOjR7NEC2PVU>
PBMC M2DCcGZ2dmO2aX;uJGF{e2G7 MmX4OVAwOTByIN88US=> NITNeHEzPCCq NFPsN4tFVVOR NXXlTmpvcW6qaXLpeJMhW1SDVEGgdIhwe3Cqb4L5cIF1cW:w MYeyOFkyOTh5Mh?=
MDA-231 Mn\XSpVv[3Srb36gRZN{[Xl? MmPUNVAxKM7:TR?= M4TyT|I1KGh? NIHFblNFVVOR MW\k[YNz\WG|ZYOgTWRQKGW6cILld5Nqd25? MVmyOFkyOTh5Mh?=
624.38mel  NXPTO3hlTnWwY4Tpc44hSXO|YYm= NGfycGE2OCEQvF2= NULofFNpOjRiaB?= NYXqNGtGTE2VTx?= MWTk[YNz\WG|ZYOgTWRQKGW6cILld5Nqd25? NF;t[3IzPDlzMUi3Ni=>
MDA-231 NWH5cll5TnWwY4Tpc44hSXO|YYm= NVn5e3NQPTBvMkCwJO69VQ>? MnTxNlQhcA>? MXLEUXNQ MWHpcohq[mm2czDJSG8h[WO2aY\peJkhcW6mZYDlcoRmdnSueTDv[kBuWk6DIHzleoVtew>? NXy5T5J4OjR7MUG4O|I>
624.38mel  NVzvfnBlTnWwY4Tpc44hSXO|YYm= NUTNSmE6PTBvMkCwJO69VQ>? NVzYbWV[OjRiaB?= MVvEUXNQ MVHpcohq[mm2czDJSG8h[WO2aY\peJkhcW6mZYDlcoRmdnSueTDv[kBuWk6DIHzleoVtew>? NHnj[YkzPDlzMUi3Ni=>
HMECs NVnwUI9CTnWwY4Tpc44hSXO|YYm= M3Xl[lExOMLizszNxsA> MmPZN|bDqGh? NEHEeIJqdmirYnn0d{BKTk8Qs9MgZY5lKEySUzDpcoR2[2WmIGPURXQyKHCqb4PwbI9zgWyjdHnvckBidmRiSWLGNUBmgHC{ZYPzbY9v NFzXZoIzPDJzMUOyOy=>
HMECs  MnG1SpVv[3Srb36gRZN{[Xl? NEHVfncyODEEoN88UeKh M4LQZlM3yqCq NY\Nb4ZocW6qaXLpeJMhUU[QzsJCpI1m\GmjdHXkJJBpd3OyaH;yfYxifGmxbjDv[kBUXEGWMTDhcoQhW1SDVEOsJIJ2fCCwb4Sgc4YhW1SDVEK= NETCZ|UzPDJzMUOyOy=>
BJAB NV\O[VJnSXCxcITvd4l{KEG|c3H5 NX;ZdnNjPcLizszN MlXJNlQhcA>? NXjxXZA6cW6mdXPld{Bk\WyuIHHwc5B1d3Orcx?= NGfaboYzPDB3N{G0Oy=>
I-83 MXfBdI9xfG:|aYOgRZN{[Xl? NHLzbIM2yqEQvF2= MmPXNlQhcA>? MVfpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M1nqblI1ODV5MUS3
NALM6 M3XFO2Fxd3C2b4Ppd{BCe3OjeR?= M3;KblXDqM7:TR?= Ml;INlQhcA>? M2e0[Ylv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NH7HU2QzPDB3N{G0Oy=>
DU-145 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT0NJE6OC1zMDFOwIcwdWx? MkLZOFghcMLi M{\WTIlvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz NWHVOIxTOjN5M{S4NVU>
Nalm-6 MV3GeY5kfGmxbjDBd5NigQ>? NVvOOI1nOTEEoN88US=> NGrYW2gyNzJxNDDo M2rtZYlv\HWlZYOgZZV1d3CqYXf5 MnLwNlM3QDF{MkO=
Reh MUDGeY5kfGmxbjDBd5NigQ>? M3zS[|ExyqEQvF2= NHvTPFMyNzJxNDDo M2fyTYlv\HWlZYOgZZV1d3CqYXf5 M13H[FI{PjhzMkKz
Nalm-6 M4j0VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfEUo5KSzVyIPMIwFEx6oDLzszN NIrI[oUzOzZ6MUKyNy=>
Reh MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fLZ2lEPTBi4pk8NVDjiIoQvF2= MUSyN|Y5OTJ{Mx?=
HEC1A NYL0WGVrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWPoPWo4OTByLUWwNEDPxE1? MlLDNlQhcA>? MYXpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> MnLINlM2QTV4OUe=
AN3CA MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTHbWZJOTByLUWwNEDPxE1? MlvWNlQhcA>? NWX1NoF3cW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? Mnq0NlM2QTV4OUe=
HEC50B MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfwdWoyODBvNUCwJO69VQ>? MYWyOEBp MWXpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> MVWyN|U6PTZ7Nx?=
HEC1A MUHBdI9xfG:|aYOgRZN{[Xl? NHH6b48zOC9zMECg{txO NX\k[lVzOjRiaB?= MYHpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NEXheIMzOzV7NU[5Oy=>
AN3CA M2ntOGFxd3C2b4Ppd{BCe3OjeR?= NVLxbGg4OjBxMUCwJO69VQ>? NYS4T5BkOjRiaB?= NVGxRWo2cW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NXLmcWl3OjN3OUW2PVc>
HEC50B NW\nUYdnSXCxcITvd4l{KEG|c3H5 NVTDRVc6OjBxMUCwJO69VQ>? NHXQeHIzPCCq NFHafXFqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NVTGd3poOjN3OUW2PVc>
EHEB MlTjRZBweHSxc3nzJGF{e2G7 NGHs[Y01OCEQvF2= MmrsNlQhcA>? NF7VVlFqdmS3Y3XzJIFxd3C2b4Ppdy=> MkjBNlM1QTdyN{W=
A549 Mn3MS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2q0Z2lEPTB;MUWuO:KyOi56INM1US=> M3zE[|I{Ozd5MUmy
A549 GAPDH-deficient MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTF6LkZCtVIvOyEEtV2= NFjCSoUzOzN5N{G5Ni=>
CLL  MX7BdI9xfG:|aYOgRZN{[Xl? MoLaNVAh|ryPwrC= M1PwbVI1NTl4IHi= M4DSd4lv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIg> MkOxNlIzODd4OE[=
MEC1 NUniNnR5SXCxcITvd4l{KEG|c3H5 Mmn0NVAxyqEQvF2= M{n1TFczKGh? MYLpcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6 MX2yNlE{Ojl5Mx?=
U937  MnG2RZBweHSxc3nzJGF{e2G7 MlO1NE45KM7:TR?= MX:0MVQ5KGh? NXnPOmpVcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NVXkdm1JOjJyN{S3NFA>
U937  NHnhU2lCeG:ydH;zbZMhSXO|YYm= M1u1bVEh|ryP M3TKNVk3KGh? NEHnd5NqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NELHNWczOjB{M{WyNy=>
Daudi NFTSXJlCeG:ydH;zbZMhSXO|YYm= MmTrNlAh|ryP NHfZW2U6PiCq NVywcIpTcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MojMNlIxOjN3MkO=
J45.01 NEPqVFRCeG:ydH;zbZMhSXO|YYm= MWWxJO69VQ>? NWfXdWNRQTZiaB?= MYnpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NUDMNI13OjJyMkO1NlM>
RPMI 8226 NH61UIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXCTWM2OD1{NT65xsDDucLiMz63JO69VQ>? NX\nSHVFOjF7NEiyOlQ>
CEM NIS0b3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\OTWM2OD1{LkVCpOKyyqByLkSg{txO NWDXd5FIOjF7NEiyOlQ>
Raji MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTy[pdKSzVyPUCuOFfDqMLzwrCwMlA1KM7:TR?= M3TYR|IyQTR6Mk[0
U937 M{Lkemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYn1S5o4UUN3ME2wMlI1yqEEsdMgNE4xPCEQvF2= NYHxN3oxOjF7NEiyOlQ>
K562 NWruZoljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGydGFWUUN3ME2wMlQ1yqEEsdMgNE4xPSEQvF2= NH;SUVIzOTl2OEK2OC=>
NALM-6 NW[wWI5qSXCxcITvd4l{KEG|c3H5 MYqxNEDPxE4EoB?= MVSyOEBp MWXpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOuaXfoeIx6 M3u4dFIyPjl7M{iz
JMV-3 MUjBdI9xfG:|aYOgRZN{[Xl? M{L6[FExKM7:TdMg NEHzVXQzPCCq NVriVI9WcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzcIlocHSueR?= NW\5NYk{OjF4OUmzPFM>
EHEB MX;GeY5kfGmxbjDBd5NigQ>? NV6zNlJVPS13MDFOwG0> NHTpS28zPCCq MkLR[IVkemWjc3XzJJAzOSCneIDy[ZN{cW:wIIPp[45q\mmlYX70cJk> Mn\qNlEyPjh|OUG=
JVM-2  M2PkcWZ2dmO2aX;uJGF{e2G7 M4DuN|MxKM7:TR?= MX6yOEBp M4jaeoRm[3KnYYPld{BxOjFiZYjwdoV{e2mxbh?= M3y2b|IyOTZ6M{mx
KBM3/Bu2506 Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXuTWMzOD1yLk[3JOK2VQ>? MVGyNFk{OzVyOR?=
KBM3/Bu2506 MlXmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjnNE43KM7:TR?= MX[yOEBp M1ryXYlv[3KnYYPld{B1cGViY3XscEBnemGldHnvckBqdiCVLYDoZZNm NFjveoEzODl|M{WwPS=>
MDA-MB-231 NH64PXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHoTWM2OD12LkCg{txO MXSyNFQ1PzN7MB?=
MCF-7 M2fCNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLsTWM2OD1zNT6wJO69VQ>? NIDibFczODR2N{O5NC=>
HLE-B3  M1[1XmZ2dmO2aX;uJGF{e2G7 NF62VGkzPSEQvF2= NX61[JN2PDhiaB?= Mom3Zoxw[2u|IFnGUk3Pu+LCk3nu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJIFv\CCLRF:g[ZhxemW|c3nvci=> MmSxNlA1OzVzNUi=
K562 MlvuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PSXVczKGh? MX;JR|UxRTNwMzDuUS=> NXvkSnBHOjB|MEexPVg>
BW-225 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NESxbmVKSzJyPUGuN|chy5dzMPMIlljDqM7:TdMg MYqxPFY3OTN6MB?=
OH-65 M3z1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrlb2hXUUN{ME2xMlM4KMPZMUFijLI5yqEQvF5CpC=> NULJVolGOTh4NkGzPFA>
GR-145 M2PFc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj6PI1KSzJyPUKuO|Qhy5diMUFijLI5KCEQvF5CpC=> NUH4N5NtOTh4NkGzPFA>
A549 NXvw[3I4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTrOFhmUUN{ME21MlQ5KMPZIEGw5qiTQCEQvF5CpC=> MkTmNVg3PjF|OEC=
CaSki  Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{L3SWlEOjB;MT6zO{DEnyBzMPMIllch|ryPwrC= NIPEdWgyQDZ4MUO4NC=>
ZMK-1 NEO5N5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUD5ZWZJUUN{ME2xMlM4KMPZIEGw5qiTPiEQvF5CpC=> MoX3NVg3PjF|OEC=
SKW6.4 NWXTUoE3SXCxcITvd4l{KEG|c3H5 NIDG[XoxNjBzLUGwJO69VQ>? MXqyOE81QCCq MVvpcoR2[2W|IHPlcIwh\GWjdHigbY4h[m:2aDD0bY1mNSCjbnSg[I9{\S1iZHXw[Y5l\W62IH3hco5meg>? NYXBfldxOThyOUKzOFA>
RPMI 8226 NVfB[YhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX[yOEBp Mn3MTWM2OD1zLkW0xsDPxE1? MXuxO|k4PjF6Nh?=
MM.1S Mm\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXu0PEBp NYm1OlI3UUN3ME2xN{41QMLizszN M2nrPFE4QTd4MUi2
MM.1R M1PHdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFuzcWg1QCCq MmTvTWM2OD1|Mz63PUDPxE1? NHS2XlEyPzl5NkG4Oi=>
U937 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXZfXY6UUN3ME2zMFIxOCEEsTC1OlAhdk1? M2PUc|E2QTNyM{[x

... 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