Forodesine hydrochloride

For research use only. Not for therapeutic Use.

  • CAT Number: I002969
  • CAS Number: 284490-13-7
  • Molecular Formula: C11H15ClN4O4
  • Molecular Weight: 302.71
  • Purity: ≥95%
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Forodesine hydrochloride (Cat No.:I002969) is a potent and selective inhibitor of purine nucleoside phosphorylase (PNP). It exerts its pharmacological activity by blocking the conversion of inosine and deoxyinosine to hypoxanthine and deoxyguanosine, respectively, leading to intracellular accumulation of these nucleosides. This disruption of purine metabolism results in T-cell-specific immunosuppression and apoptosis, making Forodesine hydrochloride a potential therapeutic agent for T-cell malignancies and autoimmune disorders. In clinical trials, Forodesine hydrochloride has demonstrated efficacy in treating cutaneous T-cell lymphoma and T-cell prolymphocytic leukemia. It is typically administered orally or intravenously and has shown manageable adverse effects, including hematological toxicities.


Catalog Number I002969
CAS Number 284490-13-7
Molecular Formula C11H15ClN4O4
Purity ≥95%
Target PNP(Purine nucleoside phosphorylase)
Solubility H2O: ≥ 74.1 mg/mL
Storage 3 years -20C powder
Related CAS 209799-67-7(free base)    
IUPAC Name 7-[(2S,3S,4R,5R)-3,4-dihydroxy-5-(hydroxymethyl)pyrrolidin-2-yl]-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one;hydrochloride
InChI InChI=1S/C11H14N4O4.ClH/c16-2-5-9(17)10(18)7(15-5)4-1-12-8-6(4)13-3-14-11(8)19;/h1,3,5,7,9-10,12,15-18H,2H2,(H,13,14,19);1H/t5-,7+,9-,10+;/m1./s1
InChIKey WEIAMZKHBCLFOG-QPAIBFMUSA-N
SMILES C1=C(C2=C(N1)C(=O)NC=N2)[C@H]3[C@@H]([C@@H]([C@H](N3)CO)O)O.Cl
Reference

1: Lewis DJ, Duvic M. Forodesine in the treatment of cutaneous T-cell lymphoma.
Expert Opin Investig Drugs. 2017 Jun;26(6):771-775. doi:
10.1080/13543784.2017.1324569. Epub 2017 May 5. Review. PubMed PMID: 28447489.

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2: Balakrishnan K, Ravandi F, Bantia S, Franklin A, Gandhi V. Preclinical and
clinical evaluation of forodesine in pediatric and adult B-cell acute
lymphoblastic leukemia. Clin Lymphoma Myeloma Leuk. 2013 Aug;13(4):458-66. doi:
10.1016/j.clml.2013.04.009. Epub 2013 Jun 15. PubMed PMID: 23773454; PubMed
Central PMCID: PMC4102435.

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3: Ogura M, Tsukasaki K, Nagai H, Uchida T, Oyama T, Suzuki T, Taguchi J,
Maruyama D, Hotta T, Tobinai K. Phase I study of BCX1777 (forodesine) in patients
with relapsed or refractory peripheral T/natural killer-cell malignancies. Cancer
Sci. 2012 Jul;103(7):1290-5. doi: 10.1111/j.1349-7006.2012.02287.x. Epub 2012 Apr
30. PubMed PMID: 22448814.

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4: Homminga I, Zwaan CM, Manz CY, Parker C, Bantia S, Smits WK, Higginbotham F,
Pieters R, Meijerink JP. In vitro efficacy of forodesine and nelarabine (ara-G)
in pediatric leukemia. Blood. 2011 Aug 25;118(8):2184-90. doi:
10.1182/blood-2011-02-337840. Epub 2011 Jul 5. PubMed PMID: 21730354.
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5: Al-Kali A, Gandhi V, Ayoubi M, Keating M, Ravandi F. Forodesine: review of
preclinical and clinical data. Future Oncol. 2010 Aug;6(8):1211-7. doi:
10.2217/fon.10.83. Review. PubMed PMID: 20799866.

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6: Korycka A, B&#322;oński JZ, Robak T. Forodesine (BCX-1777, Immucillin H)–a new
purine nucleoside analogue: mechanism of action and potential clinical
application. Mini Rev Med Chem. 2007 Sep;7(9):976-83. Review. PubMed PMID:
17897085.

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