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Rabacfosadine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rabacfosadine图片
CAS NO:859209-74-8
包装:5 mg
市场价:7000元

产品名称
GS-9219
VDC-1101
产品介绍

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].

Cas No.

859209-74-8

分子式

C21H35N8O6P

分子量

526.53

别名

GS-9219;VDC-1101;Rabacfosadine

储存和溶解度

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years