Fludarabine Phosphate

別名：F-ara-A Phosphate, NSC 118218 Phosphate

製品コード：S1229 純度：99.91%

Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

CAS No. 75607-67-9

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 44500	国内在庫あり
1g	JPY 235500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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製品安全説明書

現在のバッチを見る：純度： 99.91%

99.91

Fludarabine Phosphate関連製品

関連ターゲット	tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase	もっと見る
関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

DNA/RNA Synthesisシグナル伝達経路

DNA/RNA Synthesis阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
HL60 cells	Proliferation assay	48 h	Antiproliferative activity against human HL60 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.09 μM	25960323
MCF7 cells	Proliferation assay	48 h	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.13 μM	25960323
KG1 cells	Proliferation assay	48 h	Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.15 μM	25960323
Raji cells	Proliferation assay	48 h	Antiproliferative activity against human Raji cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM	25960323
K562 cells	Proliferation assay	48 h	Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.4 μM	25960323
ZR-75-1 cells	Proliferation assay	48 h	Antiproliferative activity against human ZR-75-1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.6 μM	25960323
MOLT3 cells	Proliferation assay	48 h	Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.95 μM	25960323
M-HeLa cells	Proliferation assay	48 h	Antiproliferative activity against human M-HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2 μM	25960323
SK-UT-1B cells	Proliferation assay	48 h	Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM	25960323
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

生物活性

製品説明

Fludarabine Phosphate is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Targets

DNA polymerase α ^[1] (Cell-free assay)	DNA polymerase δ ^[1] (Cell-free assay)
1.1 μM(Ki )	1.3 μM(Ki)

In Vitro
In vitro	Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. Fludarabine Phosphate competes with dATP for incorporation into the A site of the extending DNA strand, which results in termination of DNA strand elongation. Human DNA polymerase α incorporates more Fludarabine Phosphate into DNA than polymerase δ. Fludarabine Phosphate completively inhibits DNA polymerase α and DNA polymerase δ with K_i of 1.1 μM and 1.3 μM, respectively. DNA polymerase δ is also able to excise the incorporated Fludarabine Phosphate from DNA in vitro. ^[1]
細胞実験	細胞株	Human T lymphoblastoid cells
	濃度	30 μM
	反応時間	5 hours
	実験の流れ	Cells are incubated with Fludarabine Phosphate for 5 hr and washed twice with drug-free warm medium. 800 cells are mixed with 1.3 mL of 0.25% soft agar in Dulbecco’s medium supplemented with 20% fetal bovine serum (pre-warmed to 37 ℃) and incubated in a tissue culture dish for 10 days (humidified 5% CO₂ , 37 ℃). At the end of the incubation period, colonies of more than 40 cells are scored under a microscope. The cytotoxic effect of the drugs is expressed as a percentage of survival relative to that of untreated control cells.

In Vivo
In Vivo	Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) Fludarabine Phosphate administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. Fludarabine Phosphate administered as a single dose induces fewer number of cells surviving therapy in mice bearing P388 leukemia, accompanied by greater percentage of increase in life span (110%) and increased median survival time. ^[3]
動物実験	動物モデル	Murine Leukemia P3881
	投与量	234 mg/kg
	投与経路	A single dose i.p. at day 1

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05039892	Not yet recruiting	CholangiocarcinomaAdult	3D Medicines (Beijing) Co. Ltd.\|3D Medicines	December 2024	Phase 2
NCT05373264	Not yet recruiting	ADPKD	University Medical Center Groningen	March 2024	Phase 3

参考
[1] Huang P, et al, J Biol Chem, 1990, 265(27), 16617-16625. [2] Umbach GE, et al. Invest New Drugs, 1984, 2(3), 263-265. [3] Avramis VI, et al. Cancer Res, 1982, 42(7), 2587-2591.

参考

化学情報

分子量	365.21	化学式	C₁₀H₁₃FN₅O₇P
CAS No.	75607-67-9	SDF	Download Fludarabine Phosphate SDFをダウンロードする
Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)COP(=O)(O)O)O)O)F)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 73 mg/mL ( (199.88 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 3 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(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）μL 動物数匹

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

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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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

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):