Sapacitabine

Research use only, not for human use.

An orally available, nucleoside analog prodrug of CNDAC that interferes with DNA synthesis by causing single-strand DNA breaks.

An orally available, nucleoside analog prodrug of CNDAC that interferes with DNA synthesis by causing single-strand DNA breaks; induces arrest of the cell division cycle at G2 phase, demonstrates potent anti-tumor activity in both blood and solid tumors.Chemotherapeutic Agents Phase 3 Clinical.

Concentrations of Sapacitabine required to achieve an IC50 range from 3±0.6?μM for the colon cancer cell line HCT116 to 67±14?μM for the breast cancer cell line MDA-MB-435. Cell cycle analysis shows that 35% Sapacitabine-treated cells are arrested in late-S phase and 41% in G2/M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC50 20±6 μM).In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines.

On Day 14, the Sapacitabine (5?mg/kg)+vorinostat (33?mg/kg) group has a mean tumour volume of 245?mm3 and a tumour growth inhibition (TGI) of 92%, whereas the Sapacitabine (15?mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 107?mm3 and a TGI of 112%.

CYC-682 | CYC682

Cell Cycle/DNA Damage

Nucleoside Antimetabolite/Analog

Nucleoside Antimetabolite/Analog

Cancer

Chemotherapeutic

151823-14-2

490.64

C26H42N4O5

>98% (HPLC)

DMSO : 25 mg/mL. 50.95 mM

CCCCCCCCCCCCCCCC(NC(C=CN1[C@@H]2O[C@H](CO)[C@@H](O)[C@@H]2C#N)=NC1=O)=O

N-[1-(2-Cyano-2-deoxy-β-D-arabinofuranosyl)-1,2-dihydro-2-oxo-4-pyrimidinyl]hexadecanamide

(-20℃)

With Ice Pack

≥ 2 years