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Pentostatin

现货
Catalog No.
A3708
腺苷脱氨酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 800.00
现货
10mg
¥ 910.00
现货
50mg
¥ 4,110.00
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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.
References:
[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

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt268.27
Cas No.53910-25-1
FormulaC11H16N4O4
SynonymsDeoxycoformycin
Solubility≥13.4 mg/mL in DMSO, ≥26.8 mg/mL in H2O, <2.79 mg/mL in EtOH
Chemical Name(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
SDFDownload SDF
Canonical SMILESC1C(C(OC1N2C=NC3=C2NC=NCC3O)CO)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

培养的单核细胞,从骨髓纯化的γδ+肿瘤细胞,4例肝脾γδ+ T细胞淋巴瘤患者外周血

溶解方法

该化合物在DMSO中的溶解度大于13.4 mg/mL。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。

反应条件

10-100 μM,48 h

应用

在γδ+肿瘤T细胞中,Pentostatin(10 μM)显示早期和选择性细胞毒性作用。体外暴露于pentostatin 48小时可以减少活性CD3+/γδ+肿瘤T细胞的绝对数。Pentostatin加dAdo处理5天后,显示出正常CD3+/αβ+ T细胞持续存在。在纯化的CD3+/CD4-/CD8-γδ+肿瘤细胞中,Pentostatin(10-100μM)加dAdo的组合以剂量依赖性方式抑制克隆生长和[3H]-thymidine掺入。

动物实验 [2]:

动物模型

感染锥虫的小鼠

给药剂量

2 mg/kg

应用

在T.vanansi感染的小鼠中,Pentostatin (2 mg/kg)与cordycepin (2 mg/kg)组合使用100%有效,导致生化参数的水平有所增加,特别是肝脏酶的水平升高,伴随着肝脏和肾脏的组织病变。Pentostatin对感染组个体没有疗效

注意事项

由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。

References:

[1]. Aldinucci D, Poletto D, Zagonel V, et al. In vitro and in vivo effects of 2′‐deoxycoformycin (Pentostatin) on tumour cells from human γδ+ T‐cell malignancies[J]. British journal of haematology, 2000, 110(1): 188-196.

[2]. Dalla Rosa L, Da Silva A S, Gressler L T, et al. Cordycepin (3′-deoxyadenosine) pentostatin (deoxycoformycin) combination treatmaent of mice experimentally infected with Trypanosoma evansi[J]. Parasitology, 2013, 140(5): 663-671.

质量控制

化学结构

Pentostatin

相关生物数据

Pentostatin