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Forodesine
CAS No. 209799-67-7
Forodesine( —— )
Catalog No. M33362 CAS No. 209799-67-7
Forodesine (BCX-1777) is an orally active and potent purine nucleoside phosphorylase (PNP) inhibitor, a new purine nucleoside analog.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
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Biological Information
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Product NameForodesine
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NoteResearch use only, not for human use.
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Brief DescriptionForodesine (BCX-1777) is an orally active and potent purine nucleoside phosphorylase (PNP) inhibitor, a new purine nucleoside analog.
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DescriptionForodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.
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In VitroForodesine (10-30?μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation.Forodesine (10-30?μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) has no effect on the MM cells at 24 hours, while it could reduce the percentage of living cells in the MOLT-4 cells with 40%. Forodesine (BCX-1777), in the presence of 2'-deoxyguanosine (dGuo, 3-10 μM), inhibits human lymphocyte proliferation activated by various agents such as interleukin-2 (IL-2), mixed lymphocyte reaction (MLR) and phytohemagglutinin (PHA) (IC50 values < 0.1-0.38 μM).Cell Proliferation Assay Cell Line:Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM) Concentration:10?μM, 20?μM, 30?μM Incubation Time:24 and 48 hours Result:At the effects at 48 hours, a complete block in proliferation in the MOLT-4 cells and 15% reduction in the 5T33MM cells.Apoptosis Analysis Cell Line:Human RPMI-8226, human MOLT-4 (T-ALL) cells, 5T33MM (Multiple myeloma, MM) Concentration:10?μM, 20?μM, 30?μM Incubation Time:24 and 48 hours Result:A limited induction of apoptosis.
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In VivoForodesine (BCX-1777) has excellent oral bioavailability (63%) in mice. At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM. human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model, Forodesine is effective in prolonging the life span 2-fold or more.
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Synonyms——
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PathwayApoptosis
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TargetApoptosis
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RecptorApoptosis
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Research Area——
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Indication——
Chemical Information
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CAS Number209799-67-7
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Formula Weight266.25
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Molecular FormulaC11H14N4O4
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (375.59 mM; Ultrasonic )
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SMILESOC[C@H]1N[C@H]([C@H](O)[C@@H]1O)c1c[nH]c2c1nc[nH]c2=O
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Bieghs L, et al. The effects of forodesine in murine and human multiple myeloma cells. Adv Hematol. 2010;2010:131895.?
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