Fludarabine Phosphate

製品コードS1229 バッチS122901

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	8 mg/mL warmed with 50ºC water bath (21.9 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 is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
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]
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]

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 the drugs 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

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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Effect of opioid receptor antagonist on mitigating tumor necrosis factor-like weak inducer of apoptosis (TWEAK)-induced apoptolysis in pemphigus pathogenesis [ J Autoimmun, 2024, 149:103307]	PubMed: 39276627
Disrupting pro-survival and inflammatory pathways with dimethyl fumarate sensitizes chronic lymphocytic leukemia to cell death [ Cell Death Dis, 2024, 15(3):224]	PubMed: 38494482
A chemical probe inhibitor targeting STAT1 restricts cancer stem cell traits and angiogenesis in colorectal cancer [ J Biomed Sci, 2022, 29(1):20]	PubMed: 35313878
Z-DNA binding protein 1 mediates necroptotic and apoptotic cell death pathways in murine astrocytes following herpes simplex virus-1 infection [ J Neuroinflammation, 2022, 19(1):109]	PubMed: 35549723
MMP-10 from M1 macrophages promotes pulmonary vascular remodeling and pulmonary arterial hypertension [ Int J Biol Sci, 2022, 18(1):331-348]	PubMed: 34975336
A Drug Repurposing Screen Identifies Fludarabine Phosphate as a Potential Therapeutic Agent for N-MYC Overexpressing Neuroendocrine Prostate Cancers [ Cells, 2022, 11-142246]	PubMed: 35883689
A Drug Repurposing Screen Identifies Fludarabine Phosphate as a Potential Therapeutic Agent for N-MYC Overexpressing Neuroendocrine Prostate Cancers [ Cells, 2022, 11-142246]	PubMed: 35883689
RNase 7 Inhibits Uropathogenic Escherichia coli-Induced Inflammation in Bladder Cells under a High-Glucose Environment by Regulating the JAK/STAT Signaling Pathway [ Int J Mol Sci, 2022, 23(9)5156]	PubMed: 35563546
ABT199/venetoclax potentiates the cytotoxicity of alkylating agents and fludarabine in acute myeloid leukemia cells [ Oncotarget, 2022, 13:319-330]	PubMed: 35154579
Targeting the Non-Canonical NF-κB Pathway in Chronic Lymphocytic Leukemia and Multiple Myeloma [ Cancers (Basel), 2022, 14(6)1489]	PubMed: 35326640

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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