1. Cell Cycle/DNA Damage
  2. Nucleoside Antimetabolite/Analog

Sapacitabine (Synonyms: CS682; CYC682)

Cat. No.: HY-16445 Purity: 98.87%
Handling Instructions

Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.

For research use only. We do not sell to patients.

Sapacitabine Chemical Structure

Sapacitabine Chemical Structure

CAS No. : 151823-14-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 440 In-stock
Estimated Time of Arrival: December 31
50 mg USD 740 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1240 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Other Forms of Sapacitabine:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Sapacitabine is an orally available nucleoside analog prodrug that is structurally related to cytarabine.

IC50 & Target

nucleoside analog[1]

In Vitro

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[1].

In Vivo

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%[2].

Clinical Trial
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (50.95 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0382 mL 10.1908 mL 20.3815 mL
5 mM 0.4076 mL 2.0382 mL 4.0763 mL
10 mM 0.2038 mL 1.0191 mL 2.0382 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

A panel of colon (HT29, HCT116, COLO205, HCC2998), breast (MCF7, MDA-MB-435), lung (HOP62, HOP92), ovarian (OVCAR3, IGROV1) cancer cell lines are used in this study. The cell cycle stage and percentage of apoptotic cells are assessed by flow cytometry. In brief, cells are seeded in 25 cm3 flasks and are untreated or treated with various concentrations of Sapacitabine. At the indicated time points, adherent and non-adherent cells are collected, washed with PBS, fixed in 70% ethanol and stored at 4°C until use. Cells are rehydrated in PBS, incubated for 20 min at room temperature (25°C) with 250 μg/mL RNAse A with Triton X-100 and 20 min at 4°C with 50 μg/mL propidium iodide in the dark. The cell cycle distribution and percentage of apoptotic cells are determined with flow cytometer and analysed by FACS Calibur[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[2]

Female (nu/nu) mice are injected subcutaneously with 1×107 MV4-11 cells resuspended in 50% Matrigel at a single site on their flanks. Once tumour volumes are 126 to 256 mm3 (16 days post-implantation) animals are pair matched by tumour size into treatment groups (minimum of six mice per group) with a mean tumour size of ~190 mm3. Tumour measurements are calculated using the formula: volume (mm3)=width2 (mm)×length (mm)×0.5. Sapacitabine is administered once a day orally (5 or 15 mg/kg) for 4 days, followed by a 3-day break before another 4 days of treatment; dosing starts on the same day as distribution to the treatment groups[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

490.64

Formula

C₂₆H₄₂N₄O₅

CAS No.

151823-14-2

SMILES

O=C(N=C(NC(CCCCCCCCCCCCCCC)=O)C=C1)N1[[email protected]]2[[email protected]@H](C#N)[[email protected]](O)[[email protected]@H](CO)O2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Sapacitabine
Cat. No.:
HY-16445
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Sapacitabine

Cat. No.: HY-16445