Fludarabine

For research use only. Not for use in humans.

製品コードS1491 別名:FaraA, Fludarabinum

Fludarabine化学構造

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.

サイズ 価格(税別) 在庫  
10mM (1mL in DMSO) JPY 22900 あり
JPY 18100 あり
JPY 53400 あり
JPY 80000 あり
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文献中Selleckの製品使用例(71)

製品安全説明書

STAT阻害剤の選択性比較

生物活性

製品説明 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.
ターゲット
STAT1 [4]
(Vascular smooth muscle cells)
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jeko-1  NWfLSmVQTnWwY4Tpc44hSXO|YYm= NEXvUZEzOCEQvF2= NEnGO5IzPCCq NYDRPWh6cW6qaXLpeJMh\XiycnXzd4lwdiCxZjDJSG8> NVK1N2U5OjV7NEC3NVI>
MV-4-11 MVzBdI9xfG:|aYOgRZN{[Xl? MV:yMlUh|ryP Ml:1OFghcA>? MV;pcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= NFf5cFgzPTFzMUW4Ny=>
THP-1 MlTwRZBweHSxc3nzJGF{e2G7 Mnu4Nk42KM7:TR?= MnzEOFghcA>? M2fRTolv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NGHNXGEzPTFzMUW4Ny=>
MOLM 13 Ml3VRZBweHSxc3nzJGF{e2G7 NFzIfWgzNjVizszN NXPxRW9VPDhiaB?= MlfBbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NYDqcXFiOjVzMUG1PFM>
KBM3/Bu2506 MnvXRZBweHSxc3nzJGF{e2G7 NEfHSIEzNjVizszN NF7hPGY1QCCq M3ewbIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 MnzwNlUyOTF3OEO=
Nalm-6 MlPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIf2eHVKSzVyPUG4JO69VQ>? M1i2elI2ODZzMUCx
Reh MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTNyIN88US=> M1PGclI2ODZzMUCx
U2937 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVzJTWZoUUN3ME2xOkDPxE1? NHmyc2YzPTB4MUGwNS=>
Mec-1 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|Ux97zgNUCwJO69VQ>? NHvqPGozPTB4MUGwNS=>
RPMI-8226 NVjQUmxvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTVyMDFOwG0> M4XTeFI2ODZzMUCx
Molt-4 MneyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfhTWM2OD1zOECg{txO Mli1NlUxPjFzMEG=
Nalm-6-FluR MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFf6SWFKSzVyPUK1NEDPxE1? NWDqdWpLOjVyNkGxNFE>
Raji  MmHwSpVv[3Srb36gRZN{[Xl? M4XwdFPDqM7:TR?= NVPmdVBFOjRxNEivO|IhcA>? MYnpcoR2[2W|IHHjZ5VufWyjdHnvcpMhd2ZicEWzMEBxPjNiYX7kJJA4O8Li MV2yOFk1ODZ7NR?=
PBMC MVTGeY5kfGmxbjDBd5NigQ>? NULaSplmPTBxMUCwJO69VQ>? M3ywRVI1KGh? MlXZSG1UVw>? NHS2dXdqdmirYnn0d{BUXEGWMTDwbI9{eGixconsZZRqd25? MmrXNlQ6OTF6N{K=
MDA-231 NF;aWW1HfW6ldHnvckBCe3OjeR?= NHn0VWoyODBizszN NEDO[2UzPCCq MoToSG1UVw>? MXXk[YNz\WG|ZYOgTWRQKGW6cILld5Nqd25? MX[yOFkyOTh5Mh?=
624.38mel  NFnYXplHfW6ldHnvckBCe3OjeR?= MWq1NEDPxE1? MUOyOEBp MnPjSG1UVw>? NIrFcGJl\WO{ZXHz[ZMhUUSRIHX4dJJme3Orb36= MViyOFkyOTh5Mh?=
MDA-231 MlnoSpVv[3Srb36gRZN{[Xl? NUXucJNmPTBvMkCwJO69VQ>? NV3VdIZ[OjRiaB?= NGLwOW5FVVOR M3m1NYlvcGmkaYTzJGlFVyCjY4Tpeol1gSCrbnTldIVv\GWwdHz5JI9nKG2UTlGgcIV3\Wy| MWSyOFkyOTh5Mh?=
624.38mel  NXn4WWo1TnWwY4Tpc44hSXO|YYm= MVq1NE0zODBizszN MV2yOEBp NFmyZ|RFVVOR NIjicpdqdmirYnn0d{BKTE9iYXP0bZZqfHliaX7k[ZBmdmSnboTsfUBw\iCvUl7BJIxmfmWucx?= MoHuNlQ6OTF6N{K=
HMECs M2\jWGZ2dmO2aX;uJGF{e2G7 NIXGZ3UyODEEoN88UeKh Mn\nN|bDqGh? MmDGbY5pcWKrdIOgTWZP|rQEoHHu[EBNWFNiaX7keYNm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36gZY5lKEmURkGg[ZhxemW|c3nvci=> MlTsNlQzOTF|Mke=
HMECs  NEHYU5ZHfW6ldHnvckBCe3OjeR?= MWKxNFDDqM7:TdMg NWH0TWNIOzcEoHi= MonLbY5pcWKrdIOgTWZP|rIEoH3l[IlifGWmIIDoc5NxcG:{eXzheIlwdiCxZjDTWGFVOSCjbnSgV3RCXDNuIHL1eEBvd3Rib3[gV3RCXDJ? NYLBbIFrOjR{MUGzNlc>
BJAB Mkj1RZBweHSxc3nzJGF{e2G7 MXm1xsDPxE1? NFr4bpgzPCCq MUPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ NEPDboozPDB3N{G0Oy=>
I-83 NHzVOWhCeG:ydH;zbZMhSXO|YYm= Mni4OeKh|ryP Ml7FNlQhcA>? MmHsbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? M1PpeFI1ODV5MUS3
NALM6 MX;BdI9xfG:|aYOgRZN{[Xl? MVi1xsDPxE1? MUCyOEBp M2D3Nolv\HWlZYOgZ4VtdCCjcH;weI9{cXN? MmrSNlQxPTdzNEe=
DU-145 NX7mSHdzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3LF[lAuOTBizsznM41t NIXQS2k1QCCqwrC= NIqzZVlqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NVrE[I9ZOjN5M{S4NVU>
Nalm-6 Mk\lSpVv[3Srb36gRZN{[Xl? MmfoNVDDqM7:TR?= MX:xM|IwPCCq NW[y[2hWcW6mdXPld{BifXSxcHjh[5k> M3PkcFI{PjhzMkKz
Reh NWLqelQ5TnWwY4Tpc44hSXO|YYm= MWWxNOKh|ryP M13sV|EwOi92IHi= M2\EWYlv\HWlZYOgZZV1d3CqYXf5 M{jibVI{PjhzMkKz
Nalm-6 Ml\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoOwTWM2OCEkiMyxNQKBkc7:TR?= M1vRdVI{PjhzMkKz
Reh NVLidXJmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3z4bGlEPTBi4pk8NVDjiIoQvF2= NY\hPXRLOjN4OEGyNlM>
HEC1A NYHuc2tJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUexNFAuPTByIN88US=> MVeyOEBp MVzpcohq[mm2czDj[YxtKGe{b4f0bEBqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> NUfid29FOjN3OUW2PVc>
AN3CA NX34SoZqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUWxNFAuPTByIN88US=> MmPpNlQhcA>? NYTIfGJYcW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M2fwcVI{PTl3Nkm3
HEC50B MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULUdGlvOTByLUWwNEDPxE1? M2HXclI1KGh? MYPpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NX;U[FBZOjN3OUW2PVc>
HEC1A NH\wTZlCeG:ydH;zbZMhSXO|YYm= M1z3UVIxNzFyMDFOwG0> MYmyOEBp MVXpcoR2[2W|IHHwc5B1d3OrczDpckBiKGSxc3Wt[IVx\W6mZX70JI1idm6nch?= NF3p[WUzOzV7NU[5Oy=>
AN3CA MoHBRZBweHSxc3nzJGF{e2G7 NWeyXWhiOjBxMUCwJO69VQ>? MVyyOEBp M3zTXolv\HWlZYOgZZBweHSxc3nzJIlvKGFiZH;z[U1l\XCnbnTlcpQhdWGwbnXy NUS1fmdoOjN3OUW2PVc>
HEC50B M{C0TGFxd3C2b4Ppd{BCe3OjeR?= NXTXOmVuOjBxMUCwJO69VQ>? NHL5OJMzPCCq NETMcYtqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> MkXDNlM2QTV4OUe=
EHEB NH24OHVCeG:ydH;zbZMhSXO|YYm= MkPiOFAh|ryP M1\EfFI1KGh? MmDlbY5lfWOnczDhdI9xfG:|aYO= M1TJdFI{PDl5MEe1
A549 NVfjWoJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TucGlEPTB;MUWuO:KyOi56INM1US=> NV:2SYNZOjN|N{exPVI>
A549 GAPDH-deficient NVvEcWJLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PTRWlEPTB;MUiuOeKyOi5|INM1US=> M1e4WlI{Ozd5MUmy
CLL  NGrDPFNCeG:ydH;zbZMhSXO|YYm= NVTYenVLOTBizszNxsA> MljSNlQuQTZiaB?= MnvpbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MUCyNlIxPzZ6Nh?=
MEC1 MVjBdI9xfG:|aYOgRZN{[Xl? M2\M[FExOMLizszN MVy3NkBp MX7pcoR2[2W|IHHwc5B1d3OrczDzbYdvcW[rY3HueIx6 M1XPNVIzOTN{OUez
U937  NVfFS|VvSXCxcITvd4l{KEG|c3H5 NWrpfnVCOC56IN88US=> NVPGNmtCPC12ODDo M4[5NIlv\HWlZYOgZZBweHSxc3nzJJNtcWeqdHz5 NVjXNpJLOjJyN{S3NFA>
U937  MXrBdI9xfG:|aYOgRZN{[Xl? NGnIfmQyKM7:TR?= MVi5OkBp NUmzTI1LcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MmHwNlIxOjN3MkO=
Daudi NFTTcGxCeG:ydH;zbZMhSXO|YYm= M{fj[|IxKM7:TR?= MX65OkBp NGLucXNqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NUjXbXA1OjJyMkO1NlM>
J45.01 MVnBdI9xfG:|aYOgRZN{[Xl? M4DPUlEh|ryP Mn3UPVYhcA>? NWLMZ2hmcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NFOzN2kzOjB{M{WyNy=>
RPMI 8226 M3LMVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTJ3LkpCpOKyyqB|Lkeg{txO MmjvNlE6PDh{NkS=
CEM MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPWUFZ4UUN3ME2yMlTDqMLzwrCwMlQh|ryP M{\J[|IyQTR6Mk[0
Raji NVzTR4dRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nSTWlEPTB;MD60O:KhyrIEoECuNFQh|ryP MYWyNVk1QDJ4NB?=
U937 Mli3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTBwMkVCpOKyyqByLkC0JO69VQ>? NEfLb|YzOTl2OEK2OC=>
K562 M3jKeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnn2TWM2OD1yLkS0xsDDucLiMD6wOUDPxE1? NXz1[ZU4OjF7NEiyOlQ>
NALM-6 MXLBdI9xfG:|aYOgRZN{[Xl? M{i5S|ExKM7:TdMg NVfNdYcyOjRiaB?= MWHpcoR2[2W|IHPlcIwh[XCxcITvd4l{KHOuaXfoeIx6 NGfaNGEzOTZ7OUO4Ny=>
JMV-3 Mnn6RZBweHSxc3nzJGF{e2G7 M1vFZlExKM7:TdMg MmnGNlQhcA>? NWW3ZVhRcW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzcIlocHSueR?= MVWyNVY6QTN6Mx?=
EHEB NHf4OFVHfW6ldHnvckBCe3OjeR?= MorBOU02OCEQvF2= NIf4VlczPCCq NH\qdpdl\WO{ZXHz[ZMheDJzIHX4dJJme3Orb36gd4lodmmoaXPhcpRtgQ>? NFLEdJQzOTF4OEO5NS=>
JVM-2  Ml\2SpVv[3Srb36gRZN{[Xl? M4TxUFMxKM7:TR?= NUTZZYlrOjRiaB?= MofC[IVkemWjc3XzJJAzOSCneIDy[ZN{cW:w MlrkNlEyPjh|OUG=
KBM3/Bu2506 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|IxRTBwNkegxtVO M3v1XFIxQTN|NUC5
KBM3/Bu2506 NVLjcnFST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvQbHlkOC54IN88US=> NHHGW2UzPCCq NEPhZnlqdmO{ZXHz[ZMhfGinIHPlcIwh\nKjY4Tpc44hcW5iUz3wbIF{\Q>? NG\RfVczODl|M{WwPS=>
MDA-MB-231 NHXDSJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrjelBKSzVyPUSuNEDPxE1? NUXmfII2OjB2NEezPVA>
MCF-7 M{jwNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDqTZAxUUN3ME2xOU4xKM7:TR?= Ml7MNlA1PDd|OUC=
HLE-B3  NUnrRXBlTnWwY4Tpc44hSXO|YYm= MXOyOUDPxE1? NY\Yc|FFPDhiaB?= NVLXd3R4[myxY3vzJGlHVi4Qs,MAl4lv\HWlZXSgV3RCXDFicHjvd5Bpd3K7bHH0bY9vKGGwZDDJSG8h\XiycnXzd4lwdg>? MXGyNFQ{PTF3OB?=
K562 M4XUdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmHCO|IhcA>? NGLmUJJKSzVyPUOuN{BvVQ>? M{PPWlIxOzB5MUm4
BW-225 NFHQTmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvENIdKSzJyPUGuN|chy5dzMPMIlljDqM7:TdMg MVexPFY3OTN6MB?=
OH-65 M2HGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|IxRTFwM{egx7cyOOLKkklCpO69VcLi NHu1UWIyQDZ4MUO4NC=>
GR-145 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHLT4tKSzJyPUKuO|Qhy5diMUFijLI5KCEQvF5CpC=> NHi5c5kyQDZ4MUO4NC=>
A549 MoH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFqxfoFKSzJyPUWuOFghy5diMUFijLI5KM7:TdMg MV6xPFY3OTN6MB?=
CaSki  MmLWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3ZTIZKSzJyPUGuN|chy5diMUFijLI4KM7:TdMg M33ZPVE5PjZzM{iw
ZMK-1 NVPkeo9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnR[I02UUN{ME2xMlM4KMPZIEGw5qiTPiEQvF5CpC=> M2G0bVE5PjZzM{iw
SKW6.4 Moi4RZBweHSxc3nzJGF{e2G7 MVmwMlAyNTFyIN88US=> NWXXW4Z4OjRxNEigbC=> M4T0cIlv\HWlZYOgZ4VtdCCmZXH0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLTDk[ZBmdmSnboSgcYFvdmW{ M2LKUFE5ODl{M{Sw
RPMI 8226 MojQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVLTbZA2OjRiaB?= MonUTWM2OD1zLkW0xsDPxE1? NHeyT4oyPzl5NkG4Oi=>
MM.1S NWnyWop{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILJeXg1QCCq M{jqZ2lEPTB;MUOuOFjDqM7:TR?= MmnVNVc6PzZzOE[=
MM.1R M1GzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHKbnd7PDhiaB?= MYrJR|UxRTN|Lke5JO69VQ>? NXrnfW41OTd7N{[xPFY>
U937 Mn[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXz1U3NRUUN3ME2zMFIxOCEEsTC1OlAhdk1? Mlm5NVU6OzB|NkG=

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アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

細胞試験:

[1]

- 合併
  • 細胞株: Dexamethasone-sensitive (MM.1S) and -resistant (MM.1R) human MM cell lines, RPMI8226 and U266 cell lines
  • 濃度: 2 μg/mL
  • 反応時間: 24 hours
  • 実験の流れ:

    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.


    (参考用のみ)
動物試験:

[1]

- 合併
  • 動物モデル: Severe combined immunodeficient (SCID) mice bearing RPMI 8226 cells
  • 投薬量: 40 mg/kg
  • 投与方法: Administered via i.p.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 57 mg/mL (199.83 mM)
Water Insoluble
Ethanol Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
30% propylene glycol, 5% Tween 80, 65% D5W
混合させたのち直ちに使用することを推奨します。
30 mg/mL (suspension)

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 285.23
化学式

C10H12FN5O4

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

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

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

  • 回答:

    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.

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Tags: Fludarabineを買う | Fludarabine ic50 | Fludarabine供給者 | Fludarabineを購入する | Fludarabine費用 | Fludarabine生産者 | オーダーFludarabine | Fludarabine化学構造 | Fludarabine分子量 | Fludarabine代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID