Forodesine - CAS 209799-67-7
Catalog number:
209799-67-7
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
COA:
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Targets:
Nucleoside Antimetabolite/Analog
Description:
Forodesine, also known as BCX-1777,  is the hydrochloride salt of the synthetic high-affinity transition-state analogue forodesine. Forodesine binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction.
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Synonyms:
BCX-1777; Fodosine; Immucillin H; Immucillin-H; Fodosine.
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Current Developer:
BioCryst Pharmaceuticals Inc.
1.Preclinical and clinical evaluation of forodesine in pediatric and adult B-cell acute lymphoblastic leukemia.
Balakrishnan K1, Ravandi F, Bantia S, Franklin A, Gandhi V. Clin Lymphoma Myeloma Leuk. 2013 Aug;13(4):458-66. doi: 10.1016/j.clml.2013.04.009. Epub 2013 Jun 15.
BACKGROUND: The discovery that purine nucleoside phosphorylase (PNP) deficiency leads to T-cell lymphopenia was the basis for introducing PNP inhibitors for T-cell leukemias. Forodesine is an orally bioavailable PNP inhibitor with picomolar potency. Because T lymphoblasts and indolent chronic lymphocytic leukemia (CLL) B cells inherently elicit favorable pharmacokinetics to accumulate deoxyguanosine triphosphate (dGTP), forodesine demonstrated promising activity in preclinical and clinical settings for patients with T-cell acute lymphoblastic leukemia (T-ALL) and B-cell CLL (B-CLL). However, the use of forodesine in B-cell ALL (B-ALL) is unknown.
2.A nelarabine-resistant T-lymphoblastic leukemia CCRF-CEM variant cell line is cross-resistant to the purine nucleoside phosphorylase inhibitor forodesine.
Yamauchi T1, Uzui K2, Nishi R2, Tasaki T2, Ueda T2. Anticancer Res. 2014 Sep;34(9):4885-92.
BACKGROUND/AIM: Forodesine inhibits purine nucleoside phosphorylase, resulting in an accumulation of intracellular dGTP and consequently cell death. 9-β-D-Arabinofuranosylguanine (ara-G) is an active compound of nelarabine that is intracellularly phosphorylated to a triphosphate form, which inhibits DNA synthesis. Both agents show cytotoxicity toward T-cell malignancies. In the present study, we investigated the cytotoxicity of forodesine in vitro using ara-G-resistant leukemia cells.
3.Final results of a multicenter phase II study of the purine nucleoside phosphorylase (PNP) inhibitor forodesine in patients with advanced cutaneous T-cell lymphomas (CTCL) (Mycosis fungoides and Sézary syndrome).
Dummer R1, Duvic M2, Scarisbrick J3, Olsen EA4, Rozati S5, Eggmann N5, Goldinger SM5, Hutchinson K6, Geskin L7, Illidge TM8, Giuliano E9, Elder J10, Kim YH11. Ann Oncol. 2014 Sep;25(9):1807-12. doi: 10.1093/annonc/mdu231. Epub 2014 Jun 19.
BACKGROUND: Forodesine is a potent inhibitor of purine nucleoside phosphorylase (PNP) that leads to intracellular accumulation of deoxyguanosine triphosphate (dGTP) in T and B cells, resulting in apoptosis. Forodesine has demonstrated impressive antitumor activity in early phase clinical trials in cutaneous T-cell lymphoma (CTCL).
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CAS 209799-67-7 Forodesine

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