DFP-10917

Research use only, not for human use.

DFP-10917 (CNDAC, TAS-109) is a deoxycytidine analog with antitumor activity against various tumor cells.

DFP-10917 (CNDAC, TAS-109) is a deoxycytidine analog with antitumor activity against various tumor cells; is an orally available nucleoside analog prodrug of CNDAC, CNDAC (DFP-10917) is phosphorylated to generate its nucleotide form, functioning as a deoxycytosine mimic and is incorporated into DNA in tumor cells, causes DNA strand breaks during polymerization due to beta-elimination during the fidelity checkpoint, resulting in G2/M phase-arrest and tumor cell apoptosis.Blood Cancer Phase 2 Clinical.

Cell Viability Assay Cell Line:Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8 and XRCC3-deficient irs1SF CHO cellsConcentration:0-1 μMIncubation Time:24 hResult:Inhibited cell survival with IC50s of 0.006, 0.32, 0.48 and 0.0053 μM against Rad51D-deficient 51D1, Rad51D-complemented 51D1.3, wild-type AA8 and XRCC3-deficient irs1SF cell lines, respectively.Cell Proliferation Assay Cell Line:HL-60 and THP-1 cells Concentration:0-100 μM Incubation Time:3 days Result:Inhibited proliferation with IC50s of 1.5832 μM and 0.84 μM against HL-60 and THP-1 cells, respectively.Apoptosis Analysis Cell Line:HL-60 and THP-1 cells Concentration:0, 0.5, 1, 2, 3, 4, 5 and 10 μM Incubation Time:3, 4, 5, and 6 days Result:Induced apoptosis in both cells.Cell Cycle Analysis Cell Line:HCT116 Concentration:6?μM Incubation Time:48?h Result:36 and 36% of cells were arrested in late-S and G2/M phases, respectively.

Animal Model:CDF1 mice, P388 tumor modelDosage:20 mg/kg Administration:Intraperitoneal injection, daily for 10 daysResult:Greatly increased the survival time and survival rate.

CNDAC | TAS-109

Cell Cycle/DNA Damage

Nucleoside Antimetabolite/Analog

Nucleoside Antimetabolite/Analog

Cancer

Blood cancer

135598-68-4

252.23

C10H12N4O4

>98% (HPLC)

——

N#C[C@@H]1[C@H](N2C=CC(N)=NC2=O)O[C@H](CO)[C@H]1O

(2R,3S,4S,5R)-2-(4-amino-2-oxopyrimidin-1(2H)-yl)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-3-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years