Cytarabine

製品コードS1648 バッチS164809

印刷

化学情報

Chemical Structure Synonyms Cytarabin,Ara-C,Arabinofuranosyl Cytidine,Cytosine β-D-arabinofuranoside,Cytosine arabinoside,NSC 63878,NSC 287459,U-19920A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C9H13N3O5
分子量 243.22 CAS No. 147-94-4
Solubility (25°C)* 体外 DMSO 49 mg/mL (201.46 mM)
Water 49 mg/mL (201.46 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
Saline

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 30.000mg/ml (123.35mM) Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis.
in vitro

Cytarabine (AraC) is phosphorylated into a triphosphate form (Ara-CTP) involving deoxycytidine kinase (dCK), which competes with dCTP for incorporation into DNA, and then blocks DNA synthesis by inhibiting the function of DNA and RNA polymerases. This compound displays a higher growth inhibitory activity towards wild-type CCRF-CEM cells compared to other acute myelogenous leukemia (AML) cells with IC50 of 16 nM. [1] Increasing concentrations of this chemical (IC50 of 0.69 μM) results in decreased metabolic activity of sensitive rat leukemic cell line RO/1, and the cell toxity can be highly enhanced by transfection with human wt dCK (IC50 of 0.037 μM) but not the inactive, alternatively spliced dCK forms. [2] It apparently induces apoptosis of rat sympathetic neurons at 10 μM, of which 100 μM shows the highest toxicity and kills over 80% of the neurons by 84 hours, involving the release of mitochondrial cytochrome-c and the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by bax deletion. [3]
in vivo

Cytarabine is highly effective against acute leukaemias, which causes the characteristic G1/S blockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak dose-related fashion indicating that the use of higher dosages of this compound does not contribute to its antileukaemic effectiveness in man. [4] This chemical also causes placental growth retardation and increases placental trophoblastic cells apoptosis in the placental labyrinth zone of the pregnant Slc:Wistar rats, which increases from 3 hour after the treatment and peaks at 6 hour before returning to control levels at 48 hour, with remarkably enhanced p53 protein, p53 trancriptional target genes such as p21, cyclinG1 and fas and caspase-3 activity. [5]
特徴 The 1st of a series of cancer drugs that alters the sugar component of nucleosides.

プロトコル(参考用のみ)

キナーゼアッセイ In Vitro Growth Inhibition Assay
Stock solution of Cytarabine is prepared in absolute ethanol, and serial dilutions of this compound are prepared. CCRF-CEM cells are suspended in RPMI medium supplemented with 10% FBS, 0.1% gentamicin, and 1% sodium pyruvate. The cells are suspended in their respective media to give 10 mL volumes of cell suspension at a final density of 3-6 × 104 cells/mL. Appropriate volumes of this chemical solution are transferred to the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspended in fresh this compound -free medium, and final cell counts are determined. The data are analyzed by sigmoidal curve fitting of the cell count versus this chemical concentration, and the results are expressed as the IC50 (this compound concentration that inhibits cell growth to 50% of the control value).
細胞アッセイ 細胞株 Rat leukemic cell lines RCL/0, RO/1 and K7 and human myelomonocytic leukemic U937
濃度 ~100 μM
反応時間 24, 48 and 72 hours
実験の流れ

Cells are incubated in the presence of different concentrations of Cytarabine at 37 °C for 24, 48, and 72 hours. At the time of 20-, 44-, or 68-hour incubation in the presence of this compound, 10 mL of cell proliferation reagent WST-1 solution is added. After 2- and 4-hour incubation with WST-1, cell metabolic activity is assessed with colorimetric changes quantified by measuring the absorbance in a spectrophotometer at 450 nm. And cell division times are calculated from eosin counting in parallel with viability assay
動物実験 動物モデル Brown Norway rat with myelocytic leukaemia
投薬量 5 - 1000 mg/kg
投与方法 Injection i.v.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15832507/
  • https://pubmed.ncbi.nlm.nih.gov/11830489/
  • http://www.ncbi.nlm.nih.gov/pubmed?term=12934079
  • https://pubmed.ncbi.nlm.nih.gov/2465015/
  • http://www.ncbi.nlm.nih.gov/pubmed?term=14766721

カスタマーフィードバック

Data from [Data independently produced by , , Leukemia, 2015, 29(8): 1702–1712]

Data from [Data independently produced by , , J Exp Clin Cancer Res, 2017, 36(1):22]

Data from [Data independently produced by , , J Pharmacol Exp Ther, 2014, 350(3): 646-56]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

The ESCRT protein CHMP5 promotes T cell leukemia by enabling BRD4-p300-dependent transcription [ Nat Commun, 2025, 16(1):4133] PubMed: 40319015
Natural killer cell-derived granzyme B as a therapeutic target for alleviating graft injury during liver transplantation [ Acta Pharm Sin B, 2025, 15(10):5277-5293] PubMed: 41132839
Chidamide and cytarabine synergistically treat acute myeloid leukemia: inhibiting ribosome biogenesis via the MYC-RRP9 pathway [ Cell Death Dis, 2025, 16(1):601] PubMed: 40781078
The ADCY1-mediated cAMP signaling pathway mediates functional effects of montelukast treatment in brain organoids [ Cell Mol Life Sci, 2025, 82(1):224] PubMed: 40471331
The ADCY1-mediated cAMP signaling pathway mediates functional effects of montelukast treatment in brain organoids [ Cell Mol Life Sci, 2025, 82(1):224] PubMed: 40471331
Cysteine-reactive covalent chloro-N-acetamide ligands induce ferroptosis mediated cell death [ EMBO Rep, 2025, 10.1038/s44319-025-00593-4] PubMed: 41102521
Genome-wide CRISPR/Cas9 screen identifies AraC-daunorubicin-etoposide response modulators associated with outcomes in pediatric AML [ Blood Adv, 2025, 9(5):1078-1091] PubMed: 39715471
Mitochondrial dysfunction fuels drug resistance in adult T-cell acute lymphoblastic leukemia [ J Transl Med, 2025, 23(1):542] PubMed: 40369632
Establishment of a prognostic model based on ER stress-related cell death genes and proposing a novel combination therapy in acute myeloid leukemia [ J Transl Med, 2025, 23(1):566] PubMed: 40399990
Disulfidptosis in pediatric AML: a multi-omics approach to risk stratification and potential therapeutic strategy [ Cancer Cell Int, 2025, 25(1):199] PubMed: 40457386

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人間や獣医の診断であるか治療的な使用のためにでない。

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