1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine
1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine Basic information
- Product Name:
- 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine
- Synonyms:
-
- 1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine
- ETHYNYCYTIDINE
- ECyd
- TAS 106
- Ethynylcytidine
- 4-Amino-1-((2R,3R,4S,5R)-4-ethynyl-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one
- cytidine, 3'-c-ethynyl-
- 1-(3-C-ETHYNYL-BETA-D-RIBO-PENTOFURANOSYL)CYTOSINE
- CAS:
- 180300-43-0
- MF:
- C11H13N3O5
- MW:
- 267.24
- Product Categories:
-
- Nucleosides
- Mol File:
- 180300-43-0.mol
1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine Chemical Properties
- Melting point:
- 233-235 °C
- Boiling point:
- 536.4±60.0 °C(Predicted)
- Density
- 1.61±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:127.5(Max Conc. mg/mL);477.1(Max Conc. mM)
DMF:5.0(Max Conc. mg/mL);18.71(Max Conc. mM)
PBS (pH 7.2):10.0(Max Conc. mg/mL);37.42(Max Conc. mM) - form
- A solid
- pka
- 11.54±0.70(Predicted)
- color
- White to yellow
1-(3-C-ethynyl-β-D-ribo-pentofuranosyl)cytosine Usage And Synthesis
Uses
Ethynylcytidine, is a new nucleoside antimetabolite, and an RNA polymerase inhibitor, combined with cisplatin exhibits a potent synergistic growth-inhibitory effect via Vaults dysfunction
in vivo
In both OCUM-2MD3 and LX-1 xenografts, tumor regression is noted and a very potent antitumor effect with an tumor growth inhibition rate (IR) on day 15 of approximately 90% or even higher is observed at the minimum toxic doses of Ethynylcytidine (TAS-106) on all three administration schedules. In particular, administration of Ethynylcytidine at 6 mg/kg once weekly exhibits a marked tumor shrinking effect with an IR of 98% against the LX-1 tumor. While Ethynylcytidine treatment on an either 3 or 5 times weekly schedule has a potent antitumor effect with an IR of approximately 85%, the IR of Ethynylcytidine once weekly is less than 60% and its antitumor effect is rather weak[1].
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