Tubercidin

別名：7-deaza-adenosine

製品コード：S8095 純度：99.52%

Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

CAS No. 69-33-0

サイズ	価格(税別)	在庫状況
5mg	JPY 18100	国内在庫あり
25mg	JPY 51300	国内在庫あり
100mg	JPY 117700	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（1）

製品安全説明書

現在のバッチを見る： S809501 DMSO] 53 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度： 99.52%

99.52

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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

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
L2	Growth inhibition assay	37 uM		Growth inhibition of mouse L2 cells at 37 uM	17977728
HeLaS3	Antiviral assay		2 days	Antiviral activity against Poliovirus infected in human HeLaS3 cells assessed as inhibition of viral replication treated 1 hr before infection measured after 2 days, IC50=0.03μM	20964406
HeLaS3	Cytotoxicity assay		48 hrs	Cytotoxicity against human HeLaS3 cells after 48 hrs by celltiter-glo assay, IC50=0.4μM	20964406
HeLaS3	Cytotoxicity assay		24 hrs	Cytotoxicity against human HeLaS3 cells after 24 hrs by celltiter-glo assay, IC50=0.819μM	20964406
HeLaS3	Cytotoxicity assay		7 hrs	Cytotoxicity against human HeLaS3 cells after 7 hrs by celltiter-glo assay, IC50=1.44μM	20964406
A549	Cytostatic assay		5 days	Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.001μM	21711054
HCT116	Cytostatic assay		5 days	Cytostatic activity against human HCT116 cells after 5 days by SRB assay, GI50=0.001μM	21711054
NCI-H23	Cytostatic assay		5 days	Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.011μM	21711054
HCT15	Cytostatic assay		5 days	Cytostatic activity against human HCT15 cells after 5 days by SRB assay, GI50=0.011μM	21711054
DU145	Cytostatic assay		5 days	Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.018μM	21711054
MT4	Cytostatic assay		5 days	Cytostatic activity against human MT4 cells after 5 days by SRB assay, GI50=0.021μM	21711054
PC3	Cytostatic assay		5 days	Cytostatic activity against human PC3 cells after 5 days by SRB assay, GI50=0.048μM	21711054
Hs578	Cytostatic assay		5 days	Cytostatic activity against human Hs578 cells after 5 days by SRB assay, GI50=0.098μM	21711054
MRC5	Antitrypanosomal assay		7 days	Antitrypanosomal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 harboring beta-galactosidase infected in human MRC5 cells after 7 days by resazurin dye-based assay, EC50=0.34μM	30677668
MRC5	Cytotoxicity assay		3 days	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 3 days by resazurin dye-based assay, EC50=2.23μM	30677668
Vero	Function assay		5 days	Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-induced cytopathic effect after 5 days by MTS assay, EC50=1.3μM	31549836
L1210	Function assay			Concentration required to decrease the growth rate to 50% of control was evaluated by determining their ability to inhibit growth of L1210 cells in vitro, IC50=0.04μM	1310744
H.Ep.2	Function assay			Concentration required to decrease the growth rate to 50% of control was evaluated by determining their ability to inhibit growth of H.Ep.2 cells in vitro, IC50=0.06μM	1310744
HFF cells	Cytotoxicity assay			Cytotoxicity against uninfected human foreskin fibroblast(HFF cells), IC50=0.4μM	2846837
KB cells	Cytotoxicity assay			Cytotoxicity against human neoplastic cell line(KB cells), IC50=0.6μM	2846837
L1210	Cytotoxicity assay			In vitro cytotoxicity was evaluated against the L1210 Murine leukemic cells, IC50=0.04μM	2913300
HFF cells	Cytotoxicity assay			Cytotoxicity was evaluated against the Human diploid cells (HFF), IC50=0.3μM	2913300
H.Ep.2	Function assay			Compound was evaluated for cytotoxicity against H.Ep.-2 cells, and concentration required to inhibit the growth of treated cells to 50% of untreated control. , IC50=0.002μM	6708054
L1210	Function assay			Tested for in vitro cell growth inhibition of L1210 cells, IC50=0.043μM	8254613
H.Ep.2	Function assay			Tested for in vitro cell growth inhibition of H. Ep. 2 cells, IC50=0.06μM	8254613
HEK293	Function assay			Stabilization of Pdcd4 expressed in human HEK293 cells assessed as inhibition of TPA-induced degradation by luciferase reporter assay, IC50=0.88μM	21870828
Vero	Function assay			Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by methylene blue staining based by Plaque reduction assay, EC50=1.3μM	31549836
Vero	Function assay			Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by Alexa Fluor 488/DAPI staining based assay, EC50=1.3μM	31549836
Vero	Function assay			Inhibition of RNA-dependent RNA polymerase in Zika virus MR766 infected in African green monkey Vero cells assessed as antiviral activity by measuring reduction in virus-yield, EC50=1.3μM	31549836
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生物活性

製品説明	Tubercidin (7-deaza-adenosine), an adenosine analogue, is a nucleoside antibiotic. It is incorporated into DNA and inhibits polymerases, thereby inhibiting DNA replication and RNA and protein synthesis. This agent also exhibits antifungal and antiviral activities.

In Vitro
In vitro	Continuous exposure for 14 days to tubercidin alone is highly toxic to both human CFU-GM and BFU-E. The IC50s of tubercidin are 3.4±1.7 and 3.7±0.2 nM for CFU-GM and BFU-E, respectively. Tubercidin also has a direct dose-dependent inhibitory effect on myeloid and erythroid human bone marrow progenitor cells in vitro^[1].
細胞実験	細胞株	Human bone marrow cells
	濃度	10 nM
	反応時間	14 days
	実験の流れ	Human bone marrow cells were obtained from healthy volunteers. In the protection studies, cells are exposed to 10 nM of tubercidin in the presence or absence of various doses of NBMPR-P. Cells are continuously exposed to drugs for 14 days in a humidified atmosphere of 5% C02-95% air at 37°C. Colonies of CFU-GM (250 cells) and BFU-E (>30 hemoglobinized cells) are counted with an inverted microscope.

In Vivo
In Vivo	Tubercidin at the dose regimen (5 mg/kg everyday for 4 days) is lethal when used alone. Some of the studies show that the mortality from tubercidin is primarily due to hepatic and renal injuries and, to a lesser extent, damage to the pancreas. Coadministration of NBMPR-P at 25 mg/kg per day completely protects the mice (100% survival) from this lethal dose regimen of tubercidin^[1].
動物実験	動物モデル	CD1 mice
	投与量	5 mg/kg
	投与経路	i.p.

参考
[1] el Kouni MH, et al. Antimicrob Agents Chemother. 1989, 33(6):824-827.

参考

[1] el Kouni MH, et al. Antimicrob Agents Chemother. 1989, 33(6):824-827.

化学情報

分子量	266.25	化学式	C₁₁H₁₄N₄O₄
CAS No.	69-33-0	SDF	Download Tubercidin SDFをダウンロードする
Smiles	C1=CN(C2=NC=NC(=C21)N)C3C(C(C(O3)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 : 53 mg/mL ( (199.06 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 : Insoluble

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

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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