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Fludarabine

カタログ番号 T1038   CAS 21679-14-1
別名: NSC 118218, Fludarabinum, F-ara-A

Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.

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Fludarabine, CAS 21679-14-1
パッケージサイズ 在庫状況 単価(税別)
サンプルについてお問い合わせ
5 mg 在庫あり ¥ 11,500
10 mg 在庫あり ¥ 12,000
25 mg 在庫あり ¥ 18,500
50 mg 在庫あり ¥ 23,000
100 mg 在庫あり ¥ 32,500
200 mg 在庫あり ¥ 45,500
1 mL * 10 mM (in DMSO) 在庫あり ¥ 11,500
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生物学的特性に関する説明
化学的特性
保存条件 & 溶解度情報
説明 Fludarabine (Fludarabinum) is a fluorinated purine analog, an inhibitor of nucleic acid synthesis and an inhibitor of STAT1 activation. Fludarabine has antitumor activity and can be used for the treatment of leukemia and lymphoma.
In vitro METHODS: Multiple myeloma cells RPMI8226, MM.1S and MM.1R were treated with Fludarabine (0-64 µg/mL) for 24-48 h. Cell viability was measured by MTT Assay.
RESULTS: Fludarabine dose-time-dependently inhibited the proliferation of RPMI8226 cells with an IC50 of 1.54 µg/mL at 24 h. At 48 h, the IC50 of Fludarabine on MM.1S and MM.1R cells was 13.48 µg/mL and 33.79 µg/mL, respectively. [1]
METHODS: Rat aortic VSMCs were treated with Fludarabine (50 µM) and FBS for 30 min, and the expression levels of target proteins were detected by Western Blot.
RESULTS: FBS stimulation produced progressive JAK2 and STAT-1 activation, and Fludarabine induced a significant reduction in STAT-1 phosphorylation, while it did not alter JAK2 activation. [2]
In vivo METHODS: To assay antitumor activity in vivo, Fludarabine (8-40 mg/kg) was injected intraperitoneally into SCID mice bearing multiple myeloma RPMI8226 once daily for three days.
RESULTS: The antitumor activity of Fludarabine in vivo was demonstrated by a less than 5-fold increase in tumors treated with 40 mg/kg of Fludarabine over 25 days compared to an approximately 10-fold increase in control tumors. [1]
METHODS: To study the effect on graft-versus-host disease (GVHD), Fludarabine (0.8 mg/kg) was administered intraperitoneally to (BALB/c x C57BL/6) F1 mice harboring B-cell leukemia (BCL-1) every two weeks for five days in two cycles, followed by intraperitoneal injection of cyclophosphamide (400 mg/kg).
RESULTS: Mice treated with a Fludarabine-containing regimen prior to transplantation also had much less GVHD clinically and at necropsy, while graft-versus-leukemia appeared to be increased in the same animals. [3]
細胞研究 VSMCs were isolated from the aorta of male Wistar rats weighing ~350–500 g, as previously described. For cell culture experiments, 2 × 10^5 rat VSMCs were plated in Dulbecco's modified Eagle's medium (DMEM) with 10% fetal bovine serum (FBS). Semiconfluent VSMCs were starved by incubation in 0.5% FBS/DMEM for 36–48 h and then serum-stimulated with normal growth medium (i.e., DMEM containing 10% FBS) in the presence or absence of fludarabine (50 μM) [2].
動物実験 The animals in this study were handled according to the animal welfare regulation of the Magna Graecia University of Catanzaro, and the protocol was approved by the animal use committee of this institution. Fifty Wistar rats weighing 340 ± 40 g were anesthetized with an intramuscular injection of 100 mg/kg ketamine and 5 mg/kg xylazine. Angioplasty of the common carotid artery was performed using a balloon embolectomy catheter, as previously described and well validated in our laboratory. Fludarabine was dissolved in 30% pluronic F127 gel to the final concentrations of 2.5, 5, 15, or 25 mg/ml. At the time of balloon injury, gel containing fludarabine or vehicle was applied around the middle segment (2 cm in length) of the right injured carotid artery (0.1 ml per 1-cm length of the artery segment, equivalent to 0.5, 1, 3, or 5 mg of total fludarabine locally delivered), as previously described. As a control experiment, 200 μl of fludarabine/gel solution (25 mg/ml) were applied around the sham-operated carotid artery. To study the fludarabine toxicity, laboratory studies were performed at baseline and 2 wk after drug local delivery (25 mg/ml). Arterial pressure and heart rate were measured indirectly by a tail-cuff plethysmographic technique [2].
別名 NSC 118218, Fludarabinum, F-ara-A
分子量 285.23
分子式 C10H12FN5O4
CAS No. 21679-14-1

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

DMSO: 55 mg/mL (192.83 mM)

5% DMSO+95% Saline: 1.43 mg/mL (5 mM, precipitation)

参考文献

1. Meng H, et al. Antitumor activity of fludarabine against human multiple myeloma in vitro and in vivo. Eur J Haematol. 2007 Dec;79(6):486-93. 2. Torella D, et al. Fludarabine prevents smooth muscle proliferation in vitro and neointimal hyperplasia in vivo through specific inhibition of STAT-1 activation. Am J Physiol Heart Circ Physiol. 2007 Jun;292(6):H2935-43. 3. Weiss L, et al. Fludarabine in combination with cyclophosphamide decreases incidence of GVHD and maintains effective graft-versus-leukemia effect after allogeneic stem cell transplantation in murine lymphocytic leukemia. Bone Marrow Transplant. 2003 Jan;31(1):11-5. 4. Zhu Y, Gu H, Yang L, et al. The sequential role of Mst1/mTORC1/STAT1 activity in chemokine receptor 2-regulated B cell receptor signaling[J]. Authorea Preprints. 2021 5. Wang S, He F, Li Z, et al. Long non-coding RNA BANCR promotes interferon-β-induced cardiomyocyte apoptosis by targeting signal transducer and activator of transcription 1 in vitro[J]. International Journal of Clinical and Experimental Pathology. 2020, 13(11): 2840. 6. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells[J]. Frontiers in immunology. 2020, 11. 7. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia[J]. Cell Death & Disease. 2020, 11(2): 1-11. 8. Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation[J]. Cell Death & Differentiation. 2021: 1-18.

引用文献

1. Yang L, Li N, Yang D, et al. CCL2 regulation of MST1-mTOR-STAT1 signaling axis controls BCR signaling and B-cell differentiation. Cell Death & Differentiation. 2021: 1-18 2. Wang X, Li X, Wang J, et al. SMGL-1/NBAS acts as a RAB-8 GEF to regulate unconventional protein secretion. Journal of Cell Biology. 2022, 221(7): e202111125 3. Zhang T, Wang Y, Li Q, et al. Mesenchymal stromal cells equipped by IFNα empower T cells with potent anti-tumor immunity. Oncogene. 2022: 1-16. 4. Zhu Y, Gu H, Yang L, et al. Involvement of MST1/mTORC1/STAT1 activity in the regulation of B-cell receptor signalling by chemokine receptor 2. Clinical and Translational Medicine. 2022, 12(7): e887. 5. Chen C, Lu M, Lin S, et al. The nuclear gene rpl18 regulates erythroid maturation via JAK2-STAT3 signaling in zebrafish model of Diamond–Blackfan anemia. Cell Death & Disease. 2020, 11(2): 1-11 6. Chu K H, Lin S Y, Chiang B L. STAT6 Pathway Is Critical for the Induction and Function of Regulatory T Cells Induced by Mucosal B Cells. Frontiers in immunology. 2021 Jan 29;11:615868. doi: 10.3389/fimmu.2020.615868. eCollection 2020. 7. Wang S, He F, Li Z, et al. Long non-coding RNA BANCR promotes interferon-β-induced cardiomyocyte apoptosis by targeting signal transducer and activator of transcription 1 in vitro. International Journal of Clinical and Experimental Pathology. 2020, 13(11): 2840. 8. Ye S, Li S, Qin L, et al.GBP2 promotes clear cell renal cell carcinoma progression through immune infiltration and regulation of PD‑L1 expression via STAT1 signaling.Oncology Reports.2023, 49(3): 1-14. 9. Zhang X, Wang J, Wang M, et al.IFN-β Pretreatment Alleviates Allogeneic Renal Tubular Epithelial Cell–Induced NK Cell Responses via the IRF7/HLA-E/NKG2A Axis.The Journal of Immunology.2023 10. Zhang J, Guo H, Wang L, et al.Cediranib enhances the transcription of MHC-I by upregulating IRF-1.Biochemical Pharmacology.2024: 116036.
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関連化合物ライブラリー

この製品は下記化合物ライブラリに含まれています:
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投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください
投与量
mg/kg
動物の平均体重
g
動物あたりの投与量
ul
動物数
溶媒の組成を入力してください
% DMSO
%
% Tween 80
% ddH2O
計算する リセット

計算器

モル濃度計算機
希釈計算機
再構成計算
分子量計算機
=
X
X

モル度計算機では以下の計算が可能です

  • 既知の体積と濃度の溶液を調製するために必要な化合物の質量
  • 質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
  • 特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度
参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか?
[分子量(MW)]の欄に[197.13]と入力してください
[濃度]ボックスに10と入力し、正しい単位(millimolar)を選択します
[容量]ボックスに10と入力し、正しい単位(milliliter)を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

X
=
X

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2&V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか?
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度(開始)ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度(終了)ボックスに50を入力し正しい単位(millimolar)を選択してください
体積(終了)ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積(開始)ボックスに表示されます。

=
/

バイアルを再構成するのに必要な溶媒の量を計算する.

再構成計算機を使えば、バイアルを再構成するための試薬の量をすぐに計算することができます.
試薬の質量と目標濃度を入力するだけで計算します。

g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント:化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量(分子量)を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量(分子量)とは、物質の1分子の質量であり、統一された原子質量単位(u)で表されます。(1uは炭素12の1原子の質量の1/12に等しい)
モル質量(molar weight)とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Fludarabine 21679-14-1 Apoptosis Cell Cycle/Checkpoint DNA Damage/DNA Repair JAK/STAT signaling Stem Cells Nucleoside Antimetabolite/Analog DNA/RNA Synthesis STAT purine analogue STAT1 NSC-118218 NSC 118218 Fludarabinum Inhibitor fluorinated F-ara-A lymphoproliferative malignancies NSC118218 inhibit inhibitor