Cytarabine

別名：Cytarabin,Ara-C,Arabinofuranosyl Cytidine,Cytosine β-D-arabinofuranoside,Cytosine arabinoside,NSC 63878,NSC 287459,U-19920A

製品コード：S1648 純度：99.99%

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.

CAS No. 147-94-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
200mg	JPY 40500	国内在庫あり
1g	JPY 100500	国内在庫あり

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Cytarabine関連製品

関連ターゲット	tRNA synthetase RdRp DNA synthesis helicase ribonucleotide reductase	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Apoptosis Compound Library DNA Damage/DNA Repair compound Library Cell Cycle compound library	もっと見る

シグナル伝達経路

DNA/RNA Synthesisシグナル伝達経路

DNA/RNA Synthesis阻害剤の選択性比較

阻害剤	Citation	tRNA synthetase	RdRp	DNA synthesis	helicase	YB-1	ribonucleotide reductase	ribonucleotide reductase	PCNA	その他
ART899	0
ART812	0
ART558	0
SU056	2					+
VV116	0		+
BC-LI-0186	1	+++
Acelarin (NUC-1031)	0			++++
Suramin sodium salt	1		++							SirT1,SirT2,Topoisomerase II
ML216	3				+
Halofuginone	11	+++								Smad3
Clevudine	1
Nedaplatin	3			✔
Triapine (3-AP)	17						✔	✔
RP-6685	0
H3B-8800	0
Basic Orange 14	0
AOH1996	0								✔
Didox	0						✔	✔
Phen-DC3 Trifluoromethanesulfonate	0				✔
Robinetin	0			✔
Metarrestin	0									PNC
Brr2 Inhibitor C9	0				✔
Triglycidyl Isocyanurate (Teroxirone)	0			✔						p53
RK-33	21				✔
Oxolinic acid	0			✔						bacterial DNA gyrase,dopamine uptake
Favipiravir (T-705)	24		✔
YK-4-279	14				✔
Blasticidin S HCl	29			✔						protein synthesis
CX-3543(Quarfloxin)	0

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
KG1	Antitumor assay	100 mg/kg	11 days	Antitumor activity against human KG1 cells xenografted in mouse assessed as tumor regression at 100 mg/kg, po qd measured after 11 days post tumor implantation	26505898
L1210/0	Cytotoxicity assay		48 hrs	Cytotoxicity against mouse L1210/0 cells after 48 hrs, IC50 = 0.7 μM.	17341060
P388	Antiproliferative assay		48 hrs	Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 1.233 μM.	2778449
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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.

特性

The 1st of a series of cancer drugs that alters the sugar component of nucleosides.

Targets

DNA synthesis ^[1]
(CCRF-CEM cells)

16 nM

In Vitro
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. Cytarabine 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 Cytarabine (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] Cytarabine 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]
Kinase Assay	In Vitro Growth Inhibition Assay
Kinase Assay	Stock solution of Cytarabine is prepared in absolute ethanol, and serial dilutions of Cytarabine 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 Cytarabine solution are transferred to the cell suspensions, and incubation is continued for 72 hours. The cells are spun down and resuspended in fresh Cytarabine -free medium, and final cell counts are determined. The data are analyzed by sigmoidal curve fitting of the cell count versus Cytarabine concentration, and the results are expressed as the IC50 (Cytarabine concentration that inhibits cell growth to 50% of the control value).
細胞実験	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 Cytarabine, 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
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-mTOR / mTOR / p-S6K / S6K / p-AMPK / AMPK / p-AKT / AKT / p-ERK / ERK		24714637
	Growth inhibition assay	Cell viability		24714637

In Vivo
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 Cytarabine does not contribute to its antileukaemic effectiveness in man. ^[4] Cytarabine (250 mg/kg) 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]
動物実験	動物モデル	Brown Norway rat with myelocytic leukaemia
	投与量	5 - 1000 mg/kg
	投与経路	Injection i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05697510	Recruiting	Acute Myeloid Leukemia (AML)	Nantes University Hospital	March 16 2023	Phase 1

参考
[1] Tobias SC, et al. Mol Pharm, 2004, 1(2), 112-116. [2] Veuger MJ, et al. Blood, 2002, 99(4), 1373-1380. [3] Besirli CG, et al. Cell Death Differ, 2003, 10(9), 1045-1058. [4] Richel DJ, Br J Cancer, 1988, 58(6), 730-733. [5] Yamauchi H, et al. Biol Reprod, 2004, 70(6), 1762-1767. + 展開

参考

+ 展開

化学情報

分子量	243.22	化学式	C₉H₁₃N₃O₅
CAS No.	147-94-4	SDF	Download Cytarabine SDFをダウンロードする
Smiles	C1=CN(C(=O)N=C1N)C2C(C(C(O2)CO)O)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	１ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 49 mg/mL ( (201.46 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 49 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

Clear solution

Saline

30.0mg/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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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