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)  
JPY 20932.00
JPY 16102.00
JPY 51460.00
JPY 78020.00
JPY 161020.00

カスタマーフィードバック(4)

  • ERK signaling regulates STAT1 phosphorylation, and pSTAT1 modulates MHC II expression in the spinal cord under BCP conditions. AG490 (5 μg in 10 μL), Fludarabine (10 μg in 10 μL), or U0126 (5 μg in 10 μL) was intrathecally injected into cancer-bearing rats once a day for 14 days, beginning immediately after carcinoma cell inoculation (n = 3 in each group). (A) Representative western blot showing pSTAT1ser727, total STAT1, pERK42/44, total ERK42/44, CIITA, MHC II RTIB, and b actin protein levels in the spinal cords of BCP rats.

    Brain Behav Immun, 2017, 60:161-173. Fludarabine purchased from Selleck.

    Imatinib mesylate (IM) in combination of fludarabine phosphate (F-AMP) significantly inhibits Ki67 and c-KIT expression in GIST-T1 tumor xenografts. Tumors were collected on the day after the last treatment and were then subjected to immunohistochemical detection of Ki67 and c-KIT expression. Representative images of immunohistochemical staining of Ki67 and c-KIT in mice tumors.

    Mol Cancer Ther, 2014, 13(10): 2276-87 . Fludarabine purchased from Selleck.

  • Normal human KC pretreated with STAT1 inhibitor (fludarabine [10 uM]) or STAT3 inhibitor (STA-21 [2 uM]) for 24 h. The mRNA levels of hBD2 and hBD3 were assessed by qRT-PCR.

    Mol Cell Biol 2014 34(24), 4368-78.. Fludarabine purchased from Selleck.

    Bacterial infection in IPEC-J2 cells. The invasion and attachment of EHECO157:H7 was increased in the IPEC-J2 cells in the presence of 10 μM fludarabine. Data are expressed as the mean ± SEM (n= 6). Differences between groups were determined by paired samples t-test. *P<0.05 compared with the control.

    Int Immunopharmacol, 2016, 36:199-204.. Fludarabine purchased from Selleck.

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  M37HPGZ2dmO2aX;uJGF{e2G7 M4XtfFIxKM7:TR?= MmDKNlQhcA>? NF;BflhqdmirYnn0d{BmgHC{ZYPzbY9vKG:oIFnEUy=> NHnkZXgzPTl2MEexNi=>
MV-4-11 M1radGFxd3C2b4Ppd{BCe3OjeR?= NV;SfplJOi53IN88US=> MnXpOFghcA>? MlX6bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NEnBOYMzPTFzMUW4Ny=>
THP-1 NVLVW3ZLSXCxcITvd4l{KEG|c3H5 MWKyMlUh|ryP NInodIs1QCCq NEf2PGtqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> M{LiO|I2OTFzNUiz
MOLM 13 NYq3WmFoSXCxcITvd4l{KEG|c3H5 NHz3b4ozNjVizszN M4PpS|Q5KGh? NFLMUFJqdmS3Y3XzJIFxd3C2b4Ppd{B{dGmpaITsfS=> NYXFPY1zOjVzMUG1PFM>
KBM3/Bu2506 NVXIRY12SXCxcITvd4l{KEG|c3H5 NGjSNHQzNjVizszN NFO0Sow1QCCq MkPsbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MlTvNlUyOTF3OEO=
Nalm-6 NUTk[m1lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XDbGlEPTB;MUig{txO MXmyOVA3OTFyMR?=
Reh MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2rDNWlEPTB;M{Cg{txO MnXUNlUxPjFzMEG=
U2937 MnzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWnJR|UxRTF4IN88US=> M3SyUVI2ODZzMUCx
Mec-1 MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mlv2TWM2OO,:nkWwNEDPxE1? MmL0NlUxPjFzMEG=
RPMI-8226 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXhTWM2OD13MECg{txO NH64N|AzPTB4MUGwNS=>
Molt-4 NH3pU4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fDU2lEPTB;MUiwJO69VQ>? MYOyOVA3OTFyMR?=
Nalm-6-FluR MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHj2U4tKSzVyPUK1NEDPxE1? NG\EZ|kzPTB4MUGwNS=>
Raji  MWPGeY5kfGmxbjDBd5NigQ>? NF;hbIk{yqEQvF2= M4O3SlI1NzR6L{eyJIg> M{C5V4lv\HWlZYOgZYNkfW23bHH0bY9veyCxZjDwOVMtKHB4MzDhcoQheDd|wrC= NYjRO|NGOjR7NEC2PVU>
PBMC Mm[1SpVv[3Srb36gRZN{[Xl? NHvFRYk2OC9zMECg{txO NWXOUVBOOjRiaB?= M3jFTWROW09? MkfFbY5pcWKrdIOgV3RCXDFicHjvd5Bpd3K7bHH0bY9v NGLlNVczPDlzMUi3Ni=>
MDA-231 MWTGeY5kfGmxbjDBd5NigQ>? NUHQ[XN5OTByIN88US=> NFi2VYozPCCq NYDwWHY6TE2VTx?= NFfxS4pl\WO{ZXHz[ZMhUUSRIHX4dJJme3Orb36= MWCyOFkyOTh5Mh?=
624.38mel  NGnp[3VHfW6ldHnvckBCe3OjeR?= NUf6PJFmPTBizszN NInr[FczPCCq MXLEUXNQ NGfHdlll\WO{ZXHz[ZMhUUSRIHX4dJJme3Orb36= NXPBUlMyOjR7MUG4O|I>
MDA-231 MVvGeY5kfGmxbjDBd5NigQ>? M{mzXVUxNTJyMDFOwG0> MmGzNlQhcA>? M4TXXWROW09? M2m0WolvcGmkaYTzJGlFVyCjY4Tpeol1gSCrbnTldIVv\GWwdHz5JI9nKG2UTlGgcIV3\Wy| NHLTW5QzPDlzMUi3Ni=>
624.38mel  NGHZUGZHfW6ldHnvckBCe3OjeR?= NY\QXlcxPTBvMkCwJO69VQ>? MV:yOEBp M{XoRmROW09? M3SxZYlvcGmkaYTzJGlFVyCjY4Tpeol1gSCrbnTldIVv\GWwdHz5JI9nKG2UTlGgcIV3\Wy| M{PMXVI1QTFzOEey
HMECs MYDGeY5kfGmxbjDBd5NigQ>? MnXiNVAxyqEQvF5CpC=> MXmzOuKhcA>? NXWzPXZ6cW6qaXLpeJMhUU[QzsRCpIFv\CCOUGOgbY5lfWOnZDDTWGFVOSCyaH;zdIhwenmuYYTpc44h[W6mIFnSSlEh\XiycnXzd4lwdg>? MmPONlQzOTF|Mke=
HMECs  M2rWO2Z2dmO2aX;uJGF{e2G7 MVqxNFDDqM7:TdMg MmnMN|bDqGh? NHrDcldqdmirYnn0d{BKTk8QsdMgcYVlcWG2ZXSgdIhwe3Cqb4L5cIF1cW:wIH;mJHNVSVRzIHHu[EBUXEGWMzygZpV1KG6xdDDv[kBUXEGWMh?= NF;BZ5YzPDJzMUOyOy=>
BJAB M4KzcGFxd3C2b4Ppd{BCe3OjeR?= NGfVcmU2yqEQvF2= NHjtPXEzPCCq Ml3nbY5lfWOnczDj[YxtKGGyb4D0c5Nqew>? NXHLbZI3OjRyNUexOFc>
I-83 M4XqfGFxd3C2b4Ppd{BCe3OjeR?= NVHEeJNFPcLizszN MX:yOEBp M2f1cYlv\HWlZYOgZ4VtdCCjcH;weI9{cXN? NHL2cHkzPDB3N{G0Oy=>
NALM6 MYPBdI9xfG:|aYOgRZN{[Xl? M1rpSVXDqM7:TR?= MkL1NlQhcA>? MWrpcoR2[2W|IHPlcIwh[XCxcITvd4l{ M{fF[lI1ODV5MUS3
DU-145 M{D3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3pNE0yOCEQvHevcYw> NF7LS5E1QCCqwrC= MlTtbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NH;UXZQzOzd|NEixOS=>
Nalm-6 NYD4c2M5TnWwY4Tpc44hSXO|YYm= MmnBNVDDqM7:TR?= MXyxM|IwPCCq MojWbY5lfWOnczDheZRweGijZ4m= NXPCcFcyOjN4OEGyNlM>
Reh M4TycmZ2dmO2aX;uJGF{e2G7 NWnkUY03OTEEoN88US=> NHfEeHkyNzJxNDDo NYPndFVscW6mdXPld{BifXSxcHjh[5k> M2PlNlI{PjhzMkKz
Nalm-6 M3z3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\RfGpKSzVyIPMIwFEx6oDLzszN MV6yN|Y5OTJ{Mx?=
Reh Mor3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFS5dZdKSzVyIPMIwFEx6oDLzszN M{TwPVI{PjhzMkKz
HEC1A MnjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfmVIwyODBvNUCwJO69VQ>? M3fHTFI1KGh? NGWzTXpqdmirYnn0d{Bk\WyuIHfyc5d1cCCrbjDhJIRwe2VvZHXw[Y5l\W62IH3hco5meg>? NGHmXnczOzV7NU[5Oy=>
AN3CA MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTsRYE5OTByLUWwNEDPxE1? MknQNlQhcA>? MojQbY5pcWKrdIOgZ4VtdCCpcn;3eIghcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> MVeyN|U6PTZ7Nx?=
HEC50B NEj2T2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWKxNFAuPTByIN88US=> NYXFNYxQOjRiaB?= MWnpcohq[mm2czDj[YxtKGe{b4f0bEB{dGmpaITsfS=> NG\zbZAzOzV7NU[5Oy=>
HEC1A MYfBdI9xfG:|aYOgRZN{[Xl? Mk\jNlAwOTByIN88US=> NF3oO5czPCCq NWj6cW9ucW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> NV7ROXY6OjN3OUW2PVc>
AN3CA NHrxbW9CeG:ydH;zbZMhSXO|YYm= M4rGOFIxNzFyMDFOwG0> M1\XZ|I1KGh? NYnTUVdvcW6mdXPld{BieG:ydH;zbZMhcW5iYTDkc5NmNWSncHXu[IVvfCCvYX7u[ZI> M1jwdlI{PTl3Nkm3
HEC50B MVrBdI9xfG:|aYOgRZN{[Xl? M3H3VVIxNzFyMDFOwG0> NFv6bpczPCCq NYiyUHh1cW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MmrVNlM2QTV4OUe=
EHEB MmfmRZBweHSxc3nzJGF{e2G7 M1T1UVQxKM7:TR?= NELzXIYzPCCq NHLq[HBqdmS3Y3XzJIFxd3C2b4Ppdy=> MY[yN|Q6PzB5NR?=
A549 NV\EXmRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHwOWFKSzVyPUG1MlfDuTJwODFCuW0> Mn6wNlM{PzdzOUK=
A549 GAPDH-deficient MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTF6LkZCtVIvOyEEtV2= NFzySowzOzN5N{G5Ni=>
CLL  MkDIRZBweHSxc3nzJGF{e2G7 M3zYPFExKM7:TdMg M{L0TlI1NTl4IHi= MlXjbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bC=> Mn3jNlIzODd4OE[=
MEC1 MWnBdI9xfG:|aYOgRZN{[Xl? MX[xNFDDqM7:TR?= MoDnO|IhcA>? M4jGOolv\HWlZYOgZZBweHSxc3nzJJNq\26rZnnjZY51dHl? NIO1UoMzOjF|Mkm3Ny=>
U937  MlHhRZBweHSxc3nzJGF{e2G7 MkD6NE45KM7:TR?= MlKyOE01QCCq NY\s[XNxcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> MV[yNlA4PDdyMB?=
U937  NG\wZXZCeG:ydH;zbZMhSXO|YYm= MY[xJO69VQ>? NH;XN4c6PiCq NYjGSY8xcW6mdXPld{BieG:ydH;zbZMhe2yrZ3j0cJk> NYT1ZYdOOjJyMkO1NlM>
Daudi MnqzRZBweHSxc3nzJGF{e2G7 M3OwXVIxKM7:TR?= M4PMclk3KGh? Mmf1bY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= NWnRco4{OjJyMkO1NlM>
J45.01 NHnacYFCeG:ydH;zbZMhSXO|YYm= NILVWmwyKM7:TR?= NFPYc5A6PiCq MknJbY5lfWOnczDhdI9xfG:|aYOgd4xq\2i2bIm= MnfVNlIxOjN3MkO=
RPMI 8226 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLmSoNKSzVyPUK1MlnDqMLzwrCzMlch|ryP NXrsTFNMOjF7NEiyOlQ>
CEM NYLXeHB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISxSm5KSzVyPUKuOOKhyrIEoECuOEDPxE1? NYD4Xow{OjF7NEiyOlQ>
Raji NXfY[nR2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHWcVdKSzVyPUCuOFfDqMLzwrCwMlA1KM7:TR?= M2X3blIyQTR6Mk[0
U937 NUm5b4h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LkUGlEPTB;MD6yOOKhyrIEoECuNFQh|ryP NUXB[WxFOjF7NEiyOlQ>
K562 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwNEVCpOKyyqByLkC1JO69VQ>? NWHMNXJkOjF7NEiyOlQ>
NALM-6 NGjMNHpCeG:ydH;zbZMhSXO|YYm= NILzSVgyOCEQvF5CpC=> NFjVfoIzPCCq MoHIbY5lfWOnczDj[YxtKGGyb4D0c5NqeyC|bHnnbJRtgQ>? Moj4NlE3QTl|OEO=
JMV-3 M33qdWFxd3C2b4Ppd{BCe3OjeR?= Ml:0NVAh|ryPwrC= MUWyOEBp NEPvcZhqdmS3Y3XzJINmdGxiYYDvdJRwe2m|IIPsbYdpfGy7 MoP2NlE3QTl|OEO=
EHEB NFW2XIZHfW6ldHnvckBCe3OjeR?= MXK1MVUxKM7:TR?= MmqzNlQhcA>? MUjk[YNz\WG|ZYOgdFIyKGW6cILld5Nqd25ic3nncolncWOjboTsfS=> NX;ERY5VOjFzNkizPVE>
JVM-2  MkTrSpVv[3Srb36gRZN{[Xl? MV6zNEDPxE1? MWeyOEBp MlPS[IVkemWjc3XzJJAzOSCneIDy[ZN{cW:w M{jqZVIyOTZ6M{mx
KBM3/Bu2506 NXvR[HVqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\NfWNKSzJyPUCuOlchyrWP M3S4fVIxQTN|NUC5
KBM3/Bu2506 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWwRlUxNjZizszN M1PZSFI1KGh? NUi3VJRucW6lcnXhd4V{KHSqZTDj[YxtKG[{YXP0bY9vKGmwIGOtdIhie2V? MX[yNFk{OzVyOR?=
MDA-MB-231 NXfvOGZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUGz[|BlUUN3ME20MlAh|ryP NYjpeYVJOjB2NEezPVA>
MCF-7 M17TOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPoVnlKSzVyPUG1MlAh|ryP NHXNfIEzODR2N{O5NC=>
HLE-B3  NXeyVW9pTnWwY4Tpc44hSXO|YYm= NGXMdXIzPSEQvF2= MofEOFghcA>? MVficI9kc3NiSV\OMe6{6oDVaX7keYNm\CCVVFHUNUBxcG:|cHjvdplt[XSrb36gZY5lKEmGTzDlfJBz\XO|aX;u MlOxNlA1OzVzNUi=
K562 NXfV[|ViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjxUXVkPzJiaB?= NHnkSZBKSzVyPUOuN{BvVQ>? NXrWZWNuOjB|MEexPVg>
BW-225 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXPQPIlXUUN{ME2xMlM4KMPZMUFijLI5yqEQvF5CpC=> M{jJflE5PjZzM{iw
OH-65 NHW5ZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjuOGZHUUN{ME2xMlM4KMPZMUFijLI5yqEQvF5CpC=> M1nuZ|E5PjZzM{iw
GR-145 Ml7LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|IxRTJwN{Sgx7chOTEkiKK4JEDPxE4EoB?= Mor4NVg3PjF|OEC=
A549 M1H3emdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|IxRTVwNEigx7chOTEkiKK4JO69VcLi MX[xPFY3OTN6MB?=
CaSki  NWDaR2QxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NITVOo5KSzJyPUGuN|chy5diMUFijLI4KM7:TdMg NF\vcHEyQDZ4MUO4NC=>
ZMK-1 NVXDVWIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDHT2VKSzJyPUGuN|chy5diMUFijLI3KM7:TdMg MYWxPFY3OTN6MB?=
SKW6.4 MlLDRZBweHSxc3nzJGF{e2G7 MYGwMlAyNTFyIN88US=> MVeyOE81QCCq NVWzfm54cW6mdXPld{Bk\WyuIHTlZZRpKGmwIHLveIghfGmvZT2gZY5lKGSxc3WtJIRmeGWwZHXueEBu[W6wZYK= NHTRdVcyQDB7MkO0NC=>
RPMI 8226 NWHOboZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\mUVI1KGh? MX;JR|UxRTFwNUVCpO69VQ>? M4nHS|E4QTd4MUi2
MM.1S NVuzW3FsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml[wOFghcA>? MWnJR|UxRTF|LkS4xsDPxE1? NUC2OmZ2OTd7N{[xPFY>
MM.1R M{\k[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXFZ2I1QCCq NGHieYJKSzVyPUOzMlc6KM7:TR?= M3r2N|E4QTd4MUi2
U937 NIfXSVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG0fHRKSzVyPUOsNlAxKMLzIEW2NEBvVQ>? Mme2NVU6OzB|NkG=

多くの細胞株試験データを見る場合、クリックしてください

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]

+ 展開
  • 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]

+ 展開
  • 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:
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
別名 FaraA, Fludarabinum

便利ツール

モル濃度計算器

モル濃度計算器

解決のために必要とされるマス、ボリュームまたは濃度を計算してください。

マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • マス
    濃度
    ボリューム
    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

貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、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 ( 輸入 輸出 )

  • 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

マス 濃度 ボリューム 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01585415 Terminated Metastatic Cancer|Melanoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 9, 2012 Phase 1
NCT01503242 Recruiting Plasma Cell Myeloma|Refractory Plasma Cell Myeloma Fred Hutchinson Cancer Research Center|National Cancer Institute (NCI) January 9, 2012 Phase 1
NCT01319565 Active, not recruiting Metastatic Melanoma|Skin Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) March 9, 2011 Phase 2
NCT01145209 Active, not recruiting Small Lymphocytic Lymphoma|CLL (Chronic Lymphocytic Leukemia) National Heart, Lung, and Blood Institute (NHLBI)|University of Virginia|GlasoSmithKline|National Institutes of Health Clinical Center (CC) June 9, 2010 Phase 2
NCT02500576 Recruiting Melanoma M.D. Anderson Cancer Center|Merck Sharp & Dohme Corp.|Prometheus Inc. August 7, 2015 Phase 2
NCT01174121 Recruiting Metastatic Colorectal Cancer|Metastatic Gastric Cancer|Metastatic Pancreatic Cancer|Metastatic Hepatocellular Carcinoma|Metastatic Cholangiocarcinoma National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) July 7, 2010 Phase 2

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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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID