Sapacitabine

Name	Sapacitabine
Synonyms	CNDAC Sapacitabine 1-(2-Deoxy-2-cyano-β-D-arabinofuranosyl)cytosine 1-(2-C-Cyano-2-deoxy-β-D-arabino-pentofuranosyl)cytosine 2'-cyano-2'-deoxy-N4-palMitoyl-1-β-D-arabinofuranosyl-cytosine, sapacitabine, CYC682 4-Amino-1-[(3β-cyano-4α-hydroxy-5β-hydroxymethyltetrahydrofuran)-2β-yl]pyrimidin-2(1H)-one 1-(2-cyano-2-deoxy-β-D-arabinofuranosyl)-4-(palMitoylaMino)pyriMidin-2(1H)-one,Sapacitabine N-[1-[(2R,3S,4S,5R)-3-cyano-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-2- oxo-pyrimidin-4-yl]hexadecanamide
CAS	151823-14-2

Molecular Formula	C26H42N4O5
Molar Mass	490.64
Density	1.21±0.1 g/cm3(Predicted)
Melting Point	>177°C (dec.)
Solubility	DMSO (Slightly), Methanol (Slightly, Heated)
Appearance	Solid
Color	White to Off-White
pKa	10.04±0.20(Predicted)
Storage Condition	-20°C Freezer, Under inert atmosphere
In vitro study	Concentrations of Sapacitabine required to achieve an IC 50 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 G 2 /M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC 50 20±6 μM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines.
In vivo study	On Day 14, the Sapacitabine (5 mg/kg)+vorinostat (33 mg/kg) group has a mean tumour volume of 245 mm 3 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 mm 3 and a TGI of 112%.

biological activity	Sapacitabine are orally available nucleoside analog prodrugs and are structurally related to cytarabine.
target	nucleoside analog
in vitro study	Concentrations of Sapacitabine required to achieve an IC 50 range from 3±0.6 μ m for the colon cancer cell line HCT116 to 67±14 μ m 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 G 2 /M phase. L1210 cells with deoxycytidine kinase (dCK) activity are sensitive to Sapacitabine, (IC 50 20±6 μM). In the docetaxel/Sapacitabine combinations, synergistic effects (CI<1) are observed when docetaxel is given before Sapacitabine in both cell lines.
in vivo study	On Day 14, the Sapacitabine (5 mg/kg)+ vorinostat (33 mg/kg) group has a mean tumour volume of 245 mm 3 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 0mm 3 and a TGI of 112%.

Last Update：2024-04-09 18:58:34

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CAS: 151823-14-2
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Mobile: 18021002903
QQ: 3008007409

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