Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Rabacfosadine is a novel prodrug of the nucleotide analogue PMEG and is designed as a cytotoxic agent.
Description | Rabacfosadine is a novel prodrug of the nucleotide analogue PMEG and is designed as a cytotoxic agent. |
In vitro | 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]. |
In vivo | Rabacfosadine exhibits significant effectiveness as a sole treatment for canine lymphoma with a distinct mode of action compared to Doxorubicin. Dogs are treated with alternating doses of Rabacfosadine (1.0 mg/kg IV at weeks 0, 6, 12) and Doxorubicin (30 mg/m2 IV at weeks 3, 9, 15). Those achieving complete response (CR) undergo monthly follow-ups. Comprehensive clinicopathological evaluations, along with remission and adverse event (AE) assessments, are conducted every 21 days. The study compares the acute AEs, identified within 21 days post-initial administration of each drug, between Rabacfosadine and Doxorubicin across 46 dogs that have received at least one dose of each medication [2]. |
Synonyms | VDC-1101, GS-9219 |
Molecular Weight | 526.535 |
Formula | C21H35N8O6P |
CAS No. | 859209-74-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Rabacfosadine 859209-74-8 Others VDC1101 GS9219 GS 9219 VDC-1101 VDC 1101 GS-9219 inhibitor inhibit