Pentostatin

Pentostatin

Catalog Number:
L002368806APE
Mfr. No.:
APE-A3708
Price:
$228
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      • Overview
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          Background

          Pentostatin is a nucleoside analog and also is a potent inhibitor of adenosine deaminase. It has a broad spectrum of immunomodulatory activities. [1] The capacity of this purine analogue to inhibit proliferation and to induce apoptosis of T-cells in combination with its mild toxicity results in the approach to use pentostatin in steroid-refractory aGvHD.[2]Chronic graft-versus-host disease (GVHD) is the main cause of late morbidity and non–relapse mortality after hematopoietic stem cell transplantation (HSCT).Most relevant to GVHD, Pentostatin causes marked reduction of CD4 and CD8 cells. There is also significant B-cell depletion with reduction of IgG levels.13 This should allow it to affect GVHD at the cellular level and thus has the potential to address the many manifestations of chronic GVHD. Pentostatin is found to be active in a phase 1 study in refractory acute GVHD. A phase 2 study of pentostatin in heavily pretreated patients (median age, 33 years; median of 4 prior regimens) with chronic GVHD showed a 55% objective response rate in 58 patients.In comparison with other treatment options, pentostatin has some favourable characteristics and its effect is sustainable and the majority of responding patients survived. The costs for pentostatin are relatively low and the toxicity is moderate.

          [1]David A. Jacobsohn, Andrew L. Gilman, Alfred Rademaker et al. Evaluation of pentostatin in corticosteroid-refractory chronic graft-versus-host disease in children: a Pediatric Blood and Marrow Transplant Consortium study. BLOOD, 12 NOVEMBER 2009 _ VOLUME 114, NUMBER 20
          [2] Stefan A. Klein1, Gesine Bug2, Sabine Mousset2 et al. Long term outcome of patients with steroid-refractory acute intestinal graft versus host disease after treatment with pentostatin. British Journal of Haematology, 154, 141–155

      • Properties
        • Alternative Name
          Deoxycoformycin; (8R)-3-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7,8-dihydro-4H-imidazo[4,5-d][1,3]diazepin-8-ol
          CAS Number
          53910-25-1
          Molecular Formula
          C11H16N4O4
          Molecular Weight
          268.27
          Appearance
          A solid
          Purity
          98.76%
          Solubility
          ≥26.8 mg/mL in H2O; insoluble in EtOH; ≥13.4 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Boyd-Tressler AM, Lane GS, et al. "Up-regulated Ectonucleotidases in Fas-Associated Death Domain Protein- and Receptor-Interacting Protein Kinase 1-Deficient Jurkat Leukemia Cells Counteract Extracellular ATP/AMP Accumulation via Pannexin-1 Channels during Chemotherapeutic Drug-Induced Apoptosis." Mol Pharmacol. 2017 Jul;92(1):30-47. PMID:28461585

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