| Identification | Back Directory | [Name]
Forodesine | [CAS]
209799-67-7 | [Synonyms]
Fodosine
Isopamphos
Forodesine
Immucillin-H
BCX-1777 freebase
FORODESINE FODOSINE
(1S)-1-(9-deazahypoxanthin-9-yl)-1,4-dideoxy-1,4-iMino-D-ribitol, iMMucillin H
(1S)-1-(9-Deazahypoxanthin-9-yl)-1,4-dideoxy-1,4-imino-D-ribitol-hydrochloride
4H-Pyrrolo3,2-dpyrimidin-4-one, 7-(2S,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl-1,5-dihydro-
7-[(2S,3S,4R,5R)-3,4-Dihydroxy-5-(hydroxymethyl)-2-pyrrolidinyl]-3,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one
4H-Pyrrolo[3,2-d]pyriMidin-4-one,7-[(2S,3S,4R,5R)-3,4-dihydroxy-5-(hydroxyMethyl)-2-pyrrolidinyl]-3,5-dihydro- | [Molecular Formula]
C11H14N4O4 | [MDL Number]
MFCD09837827 | [MOL File]
209799-67-7.mol | [Molecular Weight]
266.25 |
| Chemical Properties | Back Directory | [Boiling point ]
613.5±65.0 °C(Predicted) | [density ]
2.01 | [storage temp. ]
Hygroscopic, Refrigerator, under inert atmosphere | [solubility ]
PBS (pH 7.2): 5 mg/ml | [form ]
A crystalline solid | [pka]
13.88±0.70(Predicted) | [color ]
Light brown to gray |
| Hazard Information | Back Directory | [Description]
Forodesine is a purine nucleoside analog and purine nucleoside phosphorylase (PNP) inhibitor (IC50s = 1.19, 0.48, 1.24, 0.66, and 1.57 nM for human, mouse, rat, monkey, and dog PNP, respectively). It inhibits phytohemagglutinin A-, mixed lymphocyte reaction-, or IL-2-induced proliferation of isolated human peripheral blood lymphocytes (PBLs; IC50s = <0.1-0.38 μM) in the presence, but not absence, of 2’-deoxyguanosine (dGuo). Forodesine inhibits proliferation of CEM-SS T cell acute lymphoblastic leukemia (T-ALL) cells. In vivo, forodesine (10 mg/kg) prolongs survival in the hu-PBL-SCID mouse model of xenogeneic graft versus host disease (GVHD). | [Uses]
Fodosine is a 23-pM inhibitor of bovine purine nucleoside phosphorylase (PNP) specifically designed as a transition state mimic. | [Uses]
Treatment of T-Cell malignancies such as acute lymphoblastic leukemia (ALL) and cutaneous T-cell lymphoma (CTCL) Fodosine. | [Definition]
ChEBI: Immucillin H is a pyrrolopyrimidine and a dihydroxypyrrolidine. | [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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