Pentostatin
(Synonyms: 喷司他丁; CI-825; Deoxycoformycin) 目录号 : GC12200
A purine antimetabolite and an ADA inhibitor
Cas No.:53910-25-1
Sample solution is provided at 25 µL, 10mM.
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
| Cell experiment [1]: | |
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Cell lines |
Cultured mononuclear cells and purified γδ+ tumour cells from bone marrow or peripheral blood of four patients with hepatosplenic γδ+ T-cell lymphoma |
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Preparation method |
The solubility of this compound in DMSO is >13.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10-100 μM, 48 h |
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Applications |
Pentostatin (10 μM) displayed an early and selective cytotoxic effect on γδ+ tumour T cells. After 48 h of in vitro exposure to pentostatin reduced the absolute number of viable CD3+/γδ+ tumour T cells. Exposure to pentostatin (5 days) plus dAdo revealed the persistence of normal CD3+/αβ+ T cells. Combination of pentostatin (10–100 μM) plus dAdo dose-dependently inhibited clonogenic growth and [3H]-thymidine incorporation in purified CD3+/CD4-/CD8-γδ+ tumour cells. |
| Animal experiment [2]: | |
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Animal models |
Mice infected with Trypanosoma evansi |
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Dosage form |
2 mg/kg |
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Application |
Pentostatin (2 mg/kg) in combination with cordycepin (2 mg/kg) was 100% effective in the T. evansi-infected mice. There was an increase in levels of some biochemical parameters, especially on liver enzymes, which were accompanied by histological lesions in the liver and kidneys. Pentostatin individually showed no curative effect on infected groups |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. |
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| Cas No. | 53910-25-1 | SDF | |
| 别名 | 喷司他丁; CI-825; Deoxycoformycin | ||
| 化学名 | (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 | ||
| Canonical SMILES | C1C(C(OC1N2C=NC3=C2NC=NCC3O)CO)O | ||
| 分子式 | C11H16N4O4 | 分子量 | 268.27 |
| 溶解度 | ≥ 13.4 mg/mL in DMSO, ≥ 26.8 mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7276 mL | 18.6379 mL | 37.2759 mL |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet