Cladribine

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

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.

Cladribine化学構造

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
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり
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:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(22)

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

Adenosine Deaminase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration 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
human SK-UT-1B cells Proliferation assay 48 h Antiproliferative activity against human SK-UT-1B cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=1 μM 25960323
human MCF7 cells Proliferation assay 48 h Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=45 μM 25960323
human RPMI8226 cells Proliferation assay 48 h Antiproliferative activity against human RPMI8226 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=6 μM 25960323
human KG1 cells Proliferation assay 48 h Antiproliferative activity against human KG1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=0.2 μM 25960323
human MOLT3 cells Proliferation assay 48 h Antiproliferative activity against human MOLT3 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=2.3 μM 25960323
human SKHEP1 cells Proliferation assay 48 h Antiproliferative activity against human SKHEP1 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=4 μM 25960323
human K562 cells Proliferation assay 48 h Antiproliferative activity against human K562 cells assessed as cell growth inhibition after 48 hrs by MTT assay, IC50=10 μM 25960323
human HCT116 cells Cytotoxicity assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by SRB assay, IC50=0.3 μM 25462277
human T47D cells Cytotoxicity assay 72 h Cytotoxicity against human T47D cells after 72 hrs by SRB assay, IC50=0.7 μM 25462277
human HuH7 cells Cytotoxicity assay 72 h Cytotoxicity against human HuH7 cells after 72 hrs by SRB assay, IC50=1.8 μM 25462277
human Raji cells Cytotoxicity assay 72 h Cytotoxicity against human Raji cells after 72 hrs by MTT assay, IC50=0.009 μM 21840722
CCRF-CEM cells Cytotoxicity assay 72 h Cytotoxicity against human CCRF-CEM cells after 72 hrs by MTT assay, IC50=0.0005 μM 21840722
MES-SA Cytotoxicity assay 3 days Cytotoxicity against human MES-SA cells after 3 days by MTT assay, IC50=0.165μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human paclitaxel resistant K562 cells after 3 days by MTT assay, IC50=0.17μM 21711054
P388D1 Cytotoxicity assay 3 days Cytotoxicity against mouse P388D1 cells after 3 days by MTT assay, IC50=0.285μM 21711054
CEM-DNR-bulk Cytotoxicity assay 3 days Cytotoxicity against human CEM-DNR-bulk cells after 3 days by MTT assay, IC50=0.352μM 21711054
L1210 Cytotoxicity assay 3 days Cytotoxicity against mouse L1210 cells after 3 days by MTT assay, IC50=0.393μM 21711054
EL4 Cytotoxicity assay 3 days Cytotoxicity against mouse EL4 cells after 3 days by MTT assay, IC50=0.848μM 21711054
MCF7 Cytotoxicity assay 3 days Cytotoxicity against human MCF7 cells after 3 days by MTT assay, IC50=2.35μM 21711054
K562 Cytotoxicity assay 3 days Cytotoxicity against human K562 cells after 3 days by MTT assay, IC50=7.69μM 21711054
PC3 Cytotoxicity assay 3 days Cytotoxicity against human PC3 cells after 3 days by MTT assay, IC50=8.28μM 21711054
C6 Cytotoxicity assay 3 days Cytotoxicity against rat C6 cells after 3 days by MTT assay, IC50=9.07μM 21711054
HPAC Cytotoxicity assay 3 days Cytotoxicity against human HPAC cells after 3 days by MTT assay, IC50=9.32μM 21711054
HCT116 Cytotoxicity assay 3 days Cytotoxicity against human HCT116 cells after 3 days by MTT assay, IC50=9.43μM 21711054
HT-29 Cytotoxicity assay 3 days Cytotoxicity against human HT-29 cells after 3 days by MTT assay, IC50=9.44μM 21711054
HCT116 Cytotoxicity assay 72 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=0.3μM 28219046
HuH7 Cytotoxicity assay 72 hrs Cytotoxicity against human HuH7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=1.8μM 28219046
MCF7 Cytotoxicity assay 72 hrs Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by SRB assay, IC50=2μM 28219046
P388 leukemic cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of lymphoid neoplasm P388 leukemic cell lines, ID50=0.03 μM 2995666
L1210 cell lines Function assay In vitro inhibitory effect was tested for cytostatic activity on the growth of murine leukemic L1210 cell lines, ID50=0.03 μM 2995666
L1210 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against L1210 cell lines, IC50=0.07 Μm 1732556
HEp-2 cell lines Cytotoxicity assay Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.03 μM 1732556
CCRF-CEM cell lines Cytotoxicity assay Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.003 μM 1732556
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
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
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 --

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

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

実験計算

モル濃度計算器

質量 濃度 体積 分子量

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)

mg/kg g μL

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。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Cladribineを買う | Cladribine ic50 | Cladribine供給者 | Cladribineを購入する | Cladribine費用 | Cladribine生産者 | オーダーCladribine | Cladribine化学構造 | Cladribine分子量 | Cladribine代理店