Cladribine

別名：2-CdA,2-Chloro-2′-deoxyadenosine,CldAdo,Jk 6251,NSC 105014,RWJ 26251

製品コード：S1199 純度：99.99%

Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.

CAS No. 4291-63-8

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
25mg	JPY 22000	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（24）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Cladribine関連製品

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Adenosine Deaminase阻害剤の選択性比較

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	Incubation Time	活性情報	PMID
CT26	Cytotoxicity assay	3 days	Cytotoxicity against mouse CT26 cells after 3 days by MTT assay, IC50=0.131μM	21711054
BT549	Cytotoxicity assay	3 days	Cytotoxicity against human BT549 cells after 3 days by MTT assay, IC50=0.123μM	21711054
BV173	Cytotoxicity assay	3 days	Cytotoxicity against human BV173 cells after 3 days by MTT assay, IC50=0.0008μM	21711054
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Cladribine is an adenosine deaminase inhibitor for U266, RPMI8226, and MM1.S cells with IC50 of approximately 2.43 μM, 0.75 μM, and 0.18 μM, respectively.

特性

Cladribine is primarily active in lymphoid tissues.

Targets

Adenosine deaminase (MM1.S cells) ^[1]	Adenosine deaminase (RPMI8226 cells) ^[1]	Adenosine deaminase (U266 cells) ^[1]
0.18 μM	0.75 μM	2.43 μM

In Vitro
In vitro	Cladribine exerts remarkable activity in hairy cell leukemia (HCL), a chronic B-cell lymphoproliferative disorder, producing prolonged complete remissions. Cladribine induces accumulation of DNA strand breaks, and subsequently activates the tumor suppressor p53 in lymphocytes. Cladribine may modulate STAT3 activity in MM cells. Cladribine inhibits proliferation/survival of U266, RPMI8226 and MM1.S cells in a dose-dependent manner. While U266 is the least sensitive cell line, MM1.S is the most sensitive one to cladribine. Treatment with cladribine gradually increases the percentage of cells in the G1 phase of the cell cycle and reduces the percentage of cells in S phase. Cladribine appears to increase G2-M phase in U266 cells upon 24 hour-treatment. A dose-dependent increase in apoptosis induced by cladribine is seen in both RPMI8226 and MM1.S cells. Treatment with cladribine at 0.2 μM dramatically induces activation of caspase-3, -8, and -9 and PARP cleavage in a time-dependent manner in MM1.S. Cladribine significantly decreases the phospho-STAT3 (P-STAT3) levels in a dose-dependent manner, but has no effect on the total STAT3 protein levels. ^[1] Cladribine possesses concentration-dependent apoptosis-inducing potential in the HSB2 cells. ^[2] Cladribine inhibits growth of primary mast cell (MC) and the MC line HMC-1 in a dose-dependent manner, with lower IC50 values recorded in HMC-1.2 cells harboring KIT D816V compared to HMC-1.1 cells lacking KIT D816V. ^[3] Cladribine decreases the migratory capacity of CD14⁺ monocytes, as well as of CD4⁺ and CD8⁺ T lymphocytes. ^[4]
細胞実験	細胞株	U266, RPMI8226 and MM1.S
	濃度	0 μM - 32 μM
	反応時間	72 hours
	実験の流れ	The non-radioactive cell proliferation kit is used to determine cell viability. In brief, Human MM cell line U266, RPMI8226 and MM1.S are seeded onto 96-well plates with either 0.1 mL complete medium (5% FBS) as control, or 0.1 mL of the same medium containing a series of doses of cladribine, and incubated for 72 hours. After reading all wells at 490 nm with a micro-plate reader, the percentages of surviving cells from each group relative to controls, defined as 100% survival, are determined by reduction of MTS.

In Vivo
In Vivo	Cladribine (0.7-3.5 mM) and/or diltiazem (2.4 mM), is injected intraperitoneally into adult zebrafish and red blood cell (RBC) lysates are assayed by HPLC for levels of purine nucleotides (e.g. ATP), potential biomarkers of cardiovascular health. Diltiazem increased RBC ATP concentrations, which are inhibited by co-injection of cladribine. ^[5] Plasma concentrations of Cladribine decreases rapidly following a biphasic decline after both ia and s.c. administrations. The AUC and t _1/2 beta after a single 1 mg/kg ia and 2 mg/kg s.c. injection of Cladribine are 0.66 vs 1.2 μg × h/mL and 3.5 vs 4.5 hours, respectively. ^[6]
動物実験	動物モデル	Adult wild-type (AB) zebrafish
	投与量	0.7 mM - 3.5 mM
	投与経路	Administered via i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05797740	Recruiting	Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany	August 3 2023	--
NCT04997148	Completed	Relapsing-Remitting Multiple Sclerosis	Merck Healthcare KGaA Darmstadt Germany an affiliate of Merck KGaA Darmstadt Germany\|Merck Serono Limited an affiliate of Merck KGaA Darmstadt Germany	August 11 2021	--

参考
[1] Ma J, et al. BMC Cancer. 2011, 11, 255. [2] Guchelaar HJ, et al. Cancer Chemother Pharmacol. 1998, 42(1), 77-83. [3] B?hm A, et al. Exp Hematol. 2010, 38(9), 744-755. [4] Kopadze T, et al. Eur J Neurol. 2009, 16(3), 409-412. [5] Klein LC, et al. Biomarkers. 2009, 14(8), 554-559. [6] Yeung PK, et al. Drug Metabol Drug Interact. 2008, 23(3-4), 291-298. [7] Szmigielska-Kaplon A, et al. Ann Hematol. 2002, 81(9), 508-513. + 展開

参考

+ 展開

化学情報

分子量	285.69	化学式	C₁₀H₁₂ClN₅O₃
CAS No.	4291-63-8	SDF	Download Cladribine SDFをダウンロードする
Smiles	C1C(C(OC1N2C=NC3=C(N=C(N=C32)Cl)N)CO)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 : 57 mg/mL ( (199.51 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

Clear solution

5%DMSO 1 30%PEG300 Click to order 2 1%Tween 80 Click to order 3 64%ddH2O

10.0mg/ml (35.00mM)

Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 10 μL of Tween80 to the above system, mix evenly to clarify it; then continue to add 640 μL of ddH2O to adjust the volume to 1 mL. 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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