Fludarabine (NSC 118218) Phosphate

製品コードS1229 バッチS122904

化学情報

	Synonyms	F-ara-A Phosphate, NSC 118218 Phosphate	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₁₀H₁₃FN₅O₇P
	分子量	365.21	CAS No.	75607-67-9
Solubility (25°C)*	体外	DMSO	73 mg/mL (199.88 mM)
		Water	6 mg/mL (16.42 mM)
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Fludarabine Phosphateはアデノシンおよびデオキシアデノシンのアナログであり、dATPと競合してDNAに組み込まれ、DNA/RNA Synthesisを阻害します。
in vitro	Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. This compound 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 of this chemical into DNA than polymerase δ. It 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.
in vivo	Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) of this compound administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. This chemical 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.

プロトコル(参考用のみ)

細胞アッセイ	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 this compound is expressed as a percentage of survival relative to that of untreated control cells.
動物実験	動物モデル	Murine Leukemia P3881
	投薬量	234 mg/kg
	投与方法	A single dose i.p. at day 1

参考

https://pubmed.ncbi.nlm.nih.gov/1697861/
https://pubmed.ncbi.nlm.nih.gov/6210262/
https://pubmed.ncbi.nlm.nih.gov/7083151/

カスタマーフィードバック

: Data from [Data independently produced by Mol Cancer Ther, 2014, 13(10), 2276-87]

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長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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