Network Version
Forodesine Data Sheet
| Product Name: | Forodesine |
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|---|---|---|
| CAS No.: | 209799-67-7 | |
| Cat. No.: | HY-16210 | |
| MWt: | 266.25 | |
| Formula: | C11H14N4O4 | |
| Purity : | >98% | |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
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Forodesine (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[1][2].
IC50 & Target: IC50: 1.19 nM (Human PNP), 0.48 nM (Mouse PNP), 1.24 nM (Rat PNP), 0.66 nM (Monkey PNP) and 1.57 nM (Dog PNP)[2]
In Vitro: Forodesine (10-30?μM; 24 and 48 hours; RPMI-8226, MOLT-4 and 5T33MM cells) treatment is partially inhibition of proliferation[1]. 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%[1]. 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)[2]. In Vivo: Forodesine (BCX-1777) has excellent oral bioavailability (63%) in mice[2]. At a single dose of 10 mg/kg in mice, Forodesine elevates dGuo to approximately 5 μM[2]. n the human peripheral blood lymphocyte severe combined immunodeficiency (hu-PBL-SCID) mouse model, Forodesine is effective in prolonging the life span 2-fold or more[2]. |
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