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

Sapacitabine (Synonyms: CS682; CYC682)

製品番号: HY-16445 純度: 98.51%
取扱説明書

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

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Sapacitabine 構造式

Sapacitabine 構造式

CAS 番号 : 151823-14-2

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 132 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 120 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 210 在庫あり
Estimated Time of Arrival: December 31
25 mg USD 440 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 740 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 1240 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

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製品説明

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

IC50 & Target

nucleoside analog[1]

体外実験

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].

体内実験

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].

臨床実験
分子量

490.64

分子式

C₂₆H₄₂N₄O₅

CAS 番号

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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.
参考文献
細胞実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

動物実験
[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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

参考文献
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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

SapacitabineCS682CYC682CS 682CS-682CYC 682CYC-682Nucleoside Antimetabolite/AnalogInhibitorinhibitorinhibit

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製品名:
Sapacitabine
製品番号:
HY-16445
数量:
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