5-Fluoro-2'-deoxycytidine
CAS No. : 10356-76-0
(Synonyms: FdCyd; NSC-48006)
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| 5g | $213 | In-stock |
| 25g | $959 | In-stock |
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| Cat. No. : | HY-116217 |
| M.Wt: | 245.21 |
| Formula: | C9H12FN3O4 |
| Purity: | >98 % |
| Solubility: | DMSO : 50 mg/mL (ultrasonic);H2O : 16.67 mg/mL (ultrasonic) |
5-Fluoro-2'-deoxycytidine (FdCyd), a fluoropyrimidine nucleoside analogue, is a DNA methyltransferase (DNMT) inhibitor. 5-Fluoro-2'-deoxycytidine is a tumor-selective proagent of thymidylate synthase inhibitor 5-fluoro-2′-dUMP. 5-Fluoro-2'-deoxycytidine can induce cell cycle arrest in tumor cells through the DNA damage response, and it has anti-tumor activity[1][2][3].
IC50 & Target:DNA methyltransferase (DNMT)[2]
In Vitro:5-Fluoro-2'-deoxycytidine (0-1 μM; 8-72 h) induces G2/M phase arrest in HCT116 cells by activating the DNA damage response pathway[1].
In Vivo:5-Fluoro-2'-deoxycytidine (25 mg/kg; oral administration/intravenous injection; single dose) is rapidly and sequentially converted to 5-fluoro-2'-deoxyuridine, 5-fluorouracil and 5-fluorouridine in vivo. It has low oral bioavailability, but its exposure can be increased and prolonged when combined with 3,4,5,6-tetrahydrouridine[2].
Pharmacokinetic Analysis in male CD2F1 mice[2]
| Route | Dose (mg/kg) | Cmax (μmol/L) | Tmax (min) | AUCinf (μmol/L·h) | Half-life (min) | Distribution volume (mL) | Clearance (mL/min) | % Dose in urine (0-16 h mice) | % Dose in urine (0-24 h mice) |
| i.v. | 25 | 61.8 | 5 | 18.5 | 10.4 | 30.6 | 2.05 | 1.61 | 1.94 |
| p.o. | 25 | 0.68 | 30 | 0.79 | 45.1 | / | / | / | / |