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Rabacfosadine

产品编号 T16716 CAS 859209-74-8

别名: VDC-1101, GS-9219

Rabacfosadine is a novel prodrug of the nucleotide analogue PMEG and is designed as a cytotoxic agent.

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Rabacfosadine, CAS 859209-74-8

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其他形式的 Rabacfosadine:

Rabacfosadine succinate
询价

选择批次

纯度: 99.43% ee: 100%

纯度: 98.75% ee: 100%

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	Rabacfosadine is a novel prodrug of the nucleotide analogue PMEG and is designed as a cytotoxic agent.
体外活性	Rabacfosadine inhibits the proliferation of mitogen-stimulated T and B lymphocytes (EC50: 135 and 42 nM, respectively), as determined by BrdUrd incorporation. GS-9219 has substantial antiproliferative activity against activated lymphocytes and hematopoietic tumor cell lines. Rabacfosadine is converted to its active metabolite in lymphocytes, PMEG diphosphate, via enzymatic hydrolysis, deamination, and phosphorylation. The ability of Rabacfosadine to inhibit the proliferation of activated lymphocytes and of tumor cells of hematopoietic origin is investigated. To compare the activity of GS-9219 in dividing and nondividing cells, Rabacfosadine is evaluated in these populations using a metabolism-based sodium XTT assay instead of BrdUrd assays. Results from the XTT assay displays a 127-fold difference between the EC50 values of Rabacfosadine in quiescent (EC50=17.2 μM) and proliferating (EC50=135 nM) cells. These results indicate a substantial selectivity of Rabacfosadine toward actively replicating lymphoblasts [1].
体内活性	Rabacfosadine has substantial single-agent activity in dogs with lymphoma, and a different mechanism of action than Doxorubicin. Dogs receive alternating Rabacfosadine (1.0 mg/kg IV weeks 0, 6, 12) and Doxorubicin (30 mg/m2 IV weeks 3, 9, 15). Dogs that achieved a complete response (CR) are followed by monthly evaluations. Complete clinicopathological evaluation and assessment of remission and adverse event (AEs) are performed every 21 days. Acute AEs, occurring within 21 days after administration of the first dose of each agent, are compared between Rabacfosadine and Doxorubicin in 46 dogs receiving at least 1 dose of each agent [2].

别名	VDC-1101, GS-9219
分子量	526.535
分子式	C21H35N8O6P
CAS No.	859209-74-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

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参考文献

1. Reiser H, et al. GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma. Clin Cancer Res. 2008 May 1;14(9):2824-32. 2. Thamm DH, et al. Alternating Rabacfosadine/Doxorubicin: Efficacy and Tolerability in Naïve Canine Multicentric Lymphoma. J Vet Intern Med. 2017 May;31(3):872-878.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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