MedChemExpress -Model Alovudine -25526-93-6

FromMedChemExpress LLC (MCE)

Alovudine (3'-Fluoro-3'-deoxythymidine) is a mtDNA synthesis inhibitor and a marker of DNA synthesis. Alovudine is less susceptible to inflammatory changes than 18F-Fluorodeoxyglucose (FDG) and thus is a better biomarker in pancreatic cancer. Alovudine shows anti-orthopoxvirus and anti-leukemic activity[1][2][3][4][5][6].

Alovudine

MCE China：Alovudine

Brand：MedChemExpress (MCE)

Cat. No.HY-B1516

CAS：25526-93-6

Synonyms：3'-Fluoro-3'-deoxythymidine; 3′-Deoxy-3′-fluorothymidine; FLT

Purity：99.88%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Alovudine (3'-Fluoro-3'-deoxythymidine) is a mtDNA synthesis inhibitor and a marker of DNA synthesis. Alovudine is less susceptible to inflammatory changes than 18F-Fluorodeoxyglucose (FDG) and thus is a better biomarker in pancreatic cancer. Alovudine shows anti-orthopoxvirus and anti-leukemic activity.

In Vitro：Alovudine (5-2000 nM, 6-10 days) depletes mitochondrial DNA, reduces mitochondrial encoded proteins, decreases basal oxygen consumption, decreases cell proliferation and viability, and promotes monocytic differentiationin in AML cells (OCI-AML2 and MV4-11)[3]. Alovudine significantly augmentes DNA damage in BRCA1-/- DT40 cells[4]. Alovudine (0.5-2.5 μM, 6 days) prevents spontaneous cancer cell (MDA-MB-231) metastasis, without significant toxicity[5].

In Vivo：Alovudine (50 mg/kg bid, p.o., 14 days) reduces the growth of leukemia in mouse models of human leukemia[3]. Alovudine (50-250 μM, 9 days) prevents tumour growth and metastasis in pre-clinical animals implanted into MDA-MB-231 tumour cells[5]. Alovudine (25 mg/kg (a loading dose of 25 mg/kg in 5 minutes), i.v.) reaches the extracellular fluid of the brain not by cerebrospinal fluid, but via the cerebral capillaries in rats[6].

References：

[1]. Challapalli A, et al. 3'-Deoxy-3'-¹⁸F-fluorothymidine positron emission tomography as an early predictor of disease progression in patients with advanced and metastatic pancreatic cancer. Eur J Nucl Med Mol Imaging. 2015 May;42(6):831-40. [Content Brief]

[2]. Smee DF, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52. [Content Brief]

[3]. Yehudai D, et al. The thymidine dideoxynucleoside analog, alovudine, inhibits the mitochondrial DNA polymerase γ, impairs oxidative phosphorylation and promotes monocytic differentiation in acute myeloid leukemia. Haematologica. 2019 May;104(5):963-972. [Content Brief]

[4]. Hosen Md Bayejid. Characterization of Alovudine genotoxicity and its potential implementation as an anti-cancer drug.

[5]. Mauro-Lizcano M, et al. High mitochondrial DNA content is a key determinant of stemness, proliferation, cell migration, and cancer metastasis in vivo. Cell Death Dis. 2024 Oct 11;15(10):745. [Content Brief]

[6]. Stahle L, et al. Transport of alovudine (3'-fluorothymidine) into the brain and the cerebrospinal fluid of the rat, studied by microdialysis. Life Sci. 2000 Mar 31;66(19):1805-16. [Content Brief]

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