Fludarabine

製品コードS1491 別名:FaraA, Fludarabinum

Fludarabine化学構造

分子量(MW):285.23

Fludarabine 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.

サイズ 価格(税別) 在庫  
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(33)

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 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.
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  NF2wR21HfW6ldHnvckBCe3OjeR?= NHfoWlkzOCEQvF2= MVyyOEBp MkDDbY5pcWKrdIOg[ZhxemW|c3nvckBw\iCLRF:= NHS3W5kzPTl2MEexNi=>
MV-4-11 M{nHbGFxd3C2b4Ppd{BCe3OjeR?= NYDYfXZbOi53IN88US=> MlLUOFghcA>? NGD3SWtqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> MVSyOVEyOTV6Mx?=
THP-1 MW\BdI9xfG:|aYOgRZN{[Xl? NHTXXZYzNjVizszN M4XyZ|Q5KGh? NHLReWxqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NXjtOZZMOjVzMUG1PFM>
MOLM 13 NYr1UmJrSXCxcITvd4l{KEG|c3H5 NXqwV4MyOi53IN88US=> MY[0PEBp NWKzcWJvcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NX[0cHlVOjVzMUG1PFM>
KBM3/Bu2506 M164RmFxd3C2b4Ppd{BCe3OjeR?= M{LGclIvPSEQvF2= M4nyeVQ5KGh? MoDabY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NF3LN3AzPTFzMUW4Ny=>
Nalm-6 M{foRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoC0TWM2OD1zODFOwG0> NWHkcmlIOjVyNkGxNFE>
Reh MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XMeWlEPTB;M{Cg{txO NGnXfm0zPTB4MUGwNS=>
U2937 NVTlcHR[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHmTWM2OD1zNjFOwG0> MYmyOVA3OTFyMR?=
Mec-1 NEO5fnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\KcWlEPTExvK61NFAh|ryP NVTDS45jOjVyNkGxNFE>
RPMI-8226 MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGLzU4pKSzVyPUWwNEDPxE1? MXqyOVA3OTFyMR?=
Molt-4 NFzLcmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHvLR45KSzVyPUG4NEDPxE1? NH7xPVUzPTB4MUGwNS=>
Nalm-6-FluR NGPZOm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfBRpJlUUN3ME2yOVAh|ryP MUGyOVA3OTFyMR?=
Raji  NHLESJdHfW6ldHnvckBCe3OjeR?= MX[zxsDPxE1? NIrFeHczPC92OD:3NkBp NETFTVZqdmS3Y3XzJIFk[3WvdXzheIlwdnNib3[gdFU{NCCyNkOgZY5lKHB5M9Mg MWmyOFk1ODZ7NR?=
PBMC M2PnOGZ2dmO2aX;uJGF{e2G7 NWfMRWx4PTBxMUCwJO69VQ>? MkjSNlQhcA>? NUTUb29PTE2VTx?= NYS4V4lkcW6qaXLpeJMhW1SDVEGgdIhwe3Cqb4L5cIF1cW:w NG\QXHYzPDlzMUi3Ni=>
MDA-231 NV64N4VrTnWwY4Tpc44hSXO|YYm= M4nPOlExOCEQvF2= MYCyOEBp MXjEUXNQ MkHr[IVkemWjc3XzJGlFVyCneIDy[ZN{cW:w MnOzNlQ6OTF6N{K=
624.38mel  M3HlZmZ2dmO2aX;uJGF{e2G7 MVK1NEDPxE1? MkPENlQhcA>? M2\icGROW09? MmjM[IVkemWjc3XzJGlFVyCneIDy[ZN{cW:w Mn7aNlQ6OTF6N{K=
MDA-231 MYjGeY5kfGmxbjDBd5NigQ>? MYC1NE0zODBizszN Mn\tNlQhcA>? NH70U5VFVVOR NHTpWlRqdmirYnn0d{BKTE9iYXP0bZZqfHliaX7k[ZBmdmSnboTsfUBw\iCvUl7BJIxmfmWucx?= NY\BcWt3OjR7MUG4O|I>
624.38mel  NXHrV|RmTnWwY4Tpc44hSXO|YYm= M2PjbFUxNTJyMDFOwG0> NF3jSVEzPCCq MYfEUXNQ M2LDU4lvcGmkaYTzJGlFVyCjY4Tpeol1gSCrbnTldIVv\GWwdHz5JI9nKG2UTlGgcIV3\Wy| MX[yOFkyOTh5Mh?=
HMECs M4\lc2Z2dmO2aX;uJGF{e2G7 MV[xNFDDqM7:TdMg MYqzOuKhcA>? M2TmW4lvcGmkaYTzJGlHVs7|wrDhcoQhVFCVIHnu[JVk\WRiU2TBWFEheGixc4Doc5J6dGG2aX;uJIFv\CCLUl[xJIV5eHKnc4Ppc44> NEP3OHYzPDJzMUOyOy=>
HMECs  MWjGeY5kfGmxbjDBd5NigQ>? NV;ibnN4OTBywrFOwG3DqA>? Mnu1N|bDqGh? NFW3SWxqdmirYnn0d{BKTk8QsdMgcYVlcWG2ZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIHHu[EBUXEGWMzygZpV1KG6xdDDv[kBUXEGWMh?= NVLCbGNkOjR{MUGzNlc>
BJAB M1O1c2Fxd3C2b4Ppd{BCe3OjeR?= M4\rN|XDqM7:TR?= NXHu[GNnOjRiaB?= MYHpcoR2[2W|IHPlcIwh[XCxcITvd4l{ MnLHNlQxPTdzNEe=
I-83 MWXBdI9xfG:|aYOgRZN{[Xl? M1jYOFXDqM7:TR?= M{\uW|I1KGh? MYPpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M2fJcVI1ODV5MUS3
NALM6 MUfBdI9xfG:|aYOgRZN{[Xl? NXTLTY06PcLizszN MoPBNlQhcA>? NGWybIpqdmS3Y3XzJINmdGxiYYDvdJRwe2m| NEfvVpEzPDB3N{G0Oy=>
DU-145 MnS0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGL3TosxNTFyIN88[{9udA>? NWj4TZVZPDhiaNMg NHXuPVRqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? M4\JOVI{PzN2OEG1
Nalm-6 M4DGb2Z2dmO2aX;uJGF{e2G7 NIXZUGgyOMLizszN M1PGW|EwOi92IHi= MUXpcoR2[2W|IHH1eI9xcGGpeR?= NVzTPJNxOjN4OEGyNlM>
Reh NUe1WIt{TnWwY4Tpc44hSXO|YYm= MXKxNOKh|ryP NEnzfJMyNzJxNDDo NGj4V4lqdmS3Y3XzJIF2fG:yaHHnfS=> NVXwSYk4OjN4OEGyNlM>
Nalm-6 NILmZ2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIq1cotKSzVyIPMIwFEx6oDLzszN NVnsbVd4OjN4OEGyNlM>
Reh MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fpUGlEPTBi4pk8NVDjiIoQvF2= MUOyN|Y5OTJ{Mx?=
HEC1A NXrWcoFXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPwNVAxNTVyMDFOwG0> M{XyfFI1KGh? NX;DUpNScW6qaXLpeJMh[2WubDDndo94fGhiaX6gZUBld3OnLXTldIVv\GWwdDDtZY5v\XJ? M4\ISFI{PTl3Nkm3
AN3CA NFvYNpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M12wc|ExOC13MECg{txO MmjHNlQhcA>? M13GN4lvcGmkaYTzJINmdGxiZ4Lve5RpKGmwIHGg[I9{\S2mZYDlcoRmdnRibXHucoVz MWGyN|U6PTZ7Nx?=
HEC50B MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fTSlExOC13MECg{txO M{PBUFI1KGh? NYHvUnNRcW6qaXLpeJMh[2WubDDndo94fGhic3zp[4h1dHl? MkXSNlM2QTV4OUe=
HEC1A NIXrNY1CeG:ydH;zbZMhSXO|YYm= MXuyNE8yODBizszN MXOyOEBp NFvzOZFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIHTvd4Uu\GWyZX7k[Y51KG2jbn7ldi=> Mn[5NlM2QTV4OUe=
AN3CA NGnXWItCeG:ydH;zbZMhSXO|YYm= M1fyWVIxNzFyMDFOwG0> NUfJZop2OjRiaB?= MkXsbY5lfWOnczDhdI9xfG:|aYOgbY4h[SCmb4PlMYRmeGWwZHXueEBu[W6wZYK= M{XvSVI{PTl3Nkm3
HEC50B M{PU[GFxd3C2b4Ppd{BCe3OjeR?= NUfNR4hyOjBxMUCwJO69VQ>? M2Xp[|I1KGh? NYT5fHlKcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NVXmbm9nOjN3OUW2PVc>
EHEB M13LXGFxd3C2b4Ppd{BCe3OjeR?= M3nXblQxKM7:TR?= MlX4NlQhcA>? MYrpcoR2[2W|IHHwc5B1d3Orcx?= Ml\nNlM1QTdyN{W=
A549 NUDHN21lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3HaXmlEPTB;MUWuO:KyOi56INM1US=> NGrrR20zOzN5N{G5Ni=>
A549 GAPDH-deficient MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjpZpZKSzVyPUG4MlXDuTJwMzFCuW0> MVOyN|M4PzF7Mh?=
CLL  M{\0dWFxd3C2b4Ppd{BCe3OjeR?= NUXofmtzOTBizszNxsA> NGTJN2wzPC17NjDo Mle0bY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> MkexNlIzODd4OE[=
MEC1 MUPBdI9xfG:|aYOgRZN{[Xl? MkjwNVAxyqEQvF2= MlTDO|IhcA>? MmjCbY5lfWOnczDhdI9xfG:|aYOgd4lodmmoaXPhcpRtgQ>? NXO5fW9KOjJzM{K5O|M>
U937  MXnBdI9xfG:|aYOgRZN{[Xl? NWXQcHVtOC56IN88US=> NFLCeVE1NTR6IHi= MYLpcoR2[2W|IHHwc5B1d3OrczDzcIlocHSueR?= M4DLO|IzODd2N{Cw
U937  MXfBdI9xfG:|aYOgRZN{[Xl? NXX4UlVIOSEQvF2= M2[yTlk3KGh? MnLybY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= Mnq3NlIxOjN3MkO=
Daudi MYPBdI9xfG:|aYOgRZN{[Xl? MmLKNlAh|ryP MV65OkBp NWDpRXBKcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MVyyNlAzOzV{Mx?=
J45.01 NYXSdJVvSXCxcITvd4l{KEG|c3H5 MonkNUDPxE1? M4DRXFk3KGh? Mln4bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MWqyNlAzOzV{Mx?=
RPMI 8226 M2DuTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnT6TWM2OD1{NT65xsDDucLiMz63JO69VQ>? MUKyNVk1QDJ4NB?=
CEM Mn3zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTJwNNMgxtHDqDBwNDFOwG0> M4PNe|IyQTR6Mk[0
Raji MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HvOWlEPTB;MD60O:KhyrIEoECuNFQh|ryP M2fuOFIyQTR6Mk[0
U937 MkfMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwMkVCpOKyyqByLkC0JO69VQ>? M1viNVIyQTR6Mk[0
K562 M3zsN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVjJR|UxRTBwNEVCpOKyyqByLkC1JO69VQ>? M3;0flIyQTR6Mk[0
NALM-6 MnLPRZBweHSxc3nzJGF{e2G7 M2HTe|ExKM7:TdMg M{XlelI1KGh? NWm5b|F1cW6mdXPld{Bk\WyuIHHwc5B1d3OrczDzcIlocHSueR?= NHnybJEzOTZ7OUO4Ny=>
JMV-3 MnvYRZBweHSxc3nzJGF{e2G7 NIHNVXoyOCEQvF5CpC=> NF73d3MzPCCq NGr2dmtqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPsbYdpfGy7 NHjQW5gzOTZ7OUO4Ny=>
EHEB MlPrSpVv[3Srb36gRZN{[Xl? NUS2bGpLPS13MDFOwG0> NUXZblNEOjRiaB?= MYTk[YNz\WG|ZYOgdFIyKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> MoCwNlEyPjh|OUG=
JVM-2  Mly2SpVv[3Srb36gRZN{[Xl? NYHafGFXOzBizszN MoXINlQhcA>? MoHL[IVkemWjc3XzJJAzOSCneIDy[ZN{cW:w MXqyNVE3QDN7MR?=
KBM3/Bu2506 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlLtTWMzOD1yLk[3JOK2VQ>? NGPPNWEzODl|M{WwPS=>
KBM3/Bu2506 NULsdo9TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\uTlAvPiEQvF2= MlnDNlQhcA>? NITZd3pqdmO{ZXHz[ZMhfGinIHPlcIwh\nKjY4Tpc44hcW5iUz3wbIF{\Q>? MnTZNlA6OzN3MEm=
MDA-MB-231 NISx[5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4rseWlEPTB;ND6wJO69VQ>? NEPjSlAzODR2N{O5NC=>
MCF-7 M3;pRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XVZ2lEPTB;MUWuNEDPxE1? M{LLc|IxPDR5M{mw
HLE-B3  NVnacIs{TnWwY4Tpc44hSXO|YYm= NVvBW3dzOjVizszN MYK0PEBp M3PhbIJtd2OtczDJSm4u|rQkgKPpcoR2[2WmIGPURXQyKHCqb4PwbI9zgWyjdHnvckBidmRiSVTPJIV5eHKnc4Ppc44> NFi2VWwzODR|NUG1PC=>
K562 NXnUT5NNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LlcFczKGh? Mkn6TWM2OD1|LkOgcm0> NGG2PZgzODNyN{G5PC=>
BW-225 NVr0N|lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYji[FNQUUN{ME2xMlM4KMPZMUFijLI5yqEQvF5CpC=> Mn7pNVg3PjF|OEC=
OH-65 NHLZOYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|IxRTFwM{egx7cyOOLKkklCpO69VcLi NXzFcHVIOTh4NkGzPFA>
GR-145 M4eyb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTYd5JnUUN{ME2yMlc1KMPZIEGw5qiTQCBizszNxsA> M1rMclE5PjZzM{iw
A549 M3W5Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M332OGlEOjB;NT60PEDEnyBzMPMIllgh|ryPwrC= M17vWFE5PjZzM{iw
CaSki  M3H3d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLVTWMzOD1zLkO3JOOYKDFy4pkSO{DPxE4EoB?= NELYZ4wyQDZ4MUO4NC=>
ZMK-1 NYjJcHZ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|IxRTFwM{egx7chOTEkiKK2JO69VcLi MlzVNVg3PjF|OEC=
SKW6.4 NU\o[3JCSXCxcITvd4l{KEG|c3H5 MlnPNE4xOS1zMDFOwG0> MVeyOE81QCCq M3u1T4lv\HWlZYOgZ4VtdCCmZXH0bEBqdiCkb4ToJJRqdWVvIHHu[EBld3OnLTDk[ZBmdmSnboSgcYFvdmW{ Mlq2NVgxQTJ|NEC=
RPMI 8226 M{CzdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTNTFN3OjRiaB?= NWjQWWtIUUN3ME2xMlU1yqEQvF2= NEn0fmkyPzl5NkG4Oi=>
MM.1S NHn3NHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmm2OFghcA>? NH2zS|BKSzVyPUGzMlQ5yqEQvF2= M1ThSVE4QTd4MUi2
MM.1R MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[3UoNrPDhiaB?= NX7sVW1yUUN3ME2zN{44QSEQvF2= MlTUNVc6PzZzOE[=
U937 NXjLcoRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XTNWlEPTB;MzyyNFAhyrFiNU[wJI5O NXLXfpZEOTV7M{CzOlE>

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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
  • 製剤: PBS
  • 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
保管
in solvent
別名 FaraA, Fludarabinum

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
NCT03832127 Not yet recruiting Drug: 18F-Fludarabine Myeloma Nantes University Hospital|Cyceron April 1 2019 Phase 1
NCT03348033 Enrolling by invitation Biological: Chronic Myeloid Leukemia + NK cell Chronic Myeloid Leukemia Hospital de Clinicas de Porto Alegre March 2019 Phase 1|Phase 2
NCT03613532 Recruiting Drug: Venetoclax|Drug: Fludarabine|Drug: Busulfan Acute Myeloid Leukemia (AML)|Myelodysplastic Syndrome (MDS)|Chronic Myelomonocytic Leukemia (CMML)|MDS/Myeloproliferative Neoplasm-unclassifiable (MDS/MPN-unclassifiable)|Hematopoietic Stem Cell Transplant Jacqueline Garcia MD|Dana-Farber Cancer Institute October 1 2018 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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