Fludarabine
製品コードS1491 別名：FaraA, Fludarabinum
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.
カスタマーフィードバック(5)
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Br J Cancer, 2018, 118(4):509-521. Fludarabine purchased from Selleck.
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.
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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.
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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. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| 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] |
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| 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： |
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| 動物試験： |
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溶解度 (25°C)
| 体外 | DMSO | 57 mg/mL (199.83 mM) |
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| 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 |
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| 化学式 | C10H12FN5O4 |
| CAS No. | 21679-14-1 |
| 保管 | 粉 |
| in solvent | |
| 別名 | FaraA, Fludarabinum |
便利ツール
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 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)
モル濃度計算器方程式
*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
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 )
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。
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：
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
臨床試験
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03579888 | Not yet recruiting | Acute Lymphoblastic Leukemia|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells|Blasts More Than 5 Percent of Peripheral Blood White Cells|CD19 Positive|Chronic Lymphocytic Leukemia|Minimal Residual Disease|Non-Hodgkin Lymphoma|Small Lymphocytic Lymphoma | M.D. Anderson Cancer Center|Ziopharm Oncology|Precigen Inc | December 2019 | Phase 1 |
| NCT03579888 | Not yet recruiting | Acute Lymphoblastic Leukemia|Blasts More Than 5 Percent of Bone Marrow Nucleated Cells|Blasts More Than 5 Percent of Peripheral Blood White Cells|CD19 Positive|Chronic Lymphocytic Leukemia|Minimal Residual Disease|Non-Hodgkin Lymphoma|Small Lymphocytic Lymphoma | M.D. Anderson Cancer Center|Ziopharm Oncology|Precigen Inc | December 2019 | Phase 1 |
| NCT03873805 | Not yet recruiting | Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma|PSA Progression|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 | City of Hope Medical Center|National Cancer Institute (NCI) | August 1 2019 | Phase 1 |
| NCT03873805 | Not yet recruiting | Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma|PSA Progression|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8 | City of Hope Medical Center|National Cancer Institute (NCI) | August 1 2019 | Phase 1 |
| NCT03710421 | Not yet recruiting | Recurrent Plasma Cell Myeloma|Refractory Plasma Cell Myeloma | City of Hope Medical Center|National Cancer Institute (NCI) | June 10 2019 | Phase 1 |
| NCT03856216 | Not yet recruiting | Acute Lymphoblastic Leukemia|Allogeneic Hematopoietic Stem Cell Transplantation Recipient|B Acute Lymphoblastic Leukemia|CD22 Positive|Lymphocytic Neoplasm|Lymphoma | M.D. Anderson Cancer Center|National Cancer Institute (NCI) | June 30 2019 | 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。
他に質問がある場合は、お気軽にお問い合わせください。
よくある質問（FAQ）
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質問1：
how to re-suspend and deliver the inhibitor for in vivo experiments?
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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.
