Clofarabine

別名：Clolar

製品コード：S1218 純度：99.90%

Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.

CAS No. 123318-82-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 55500	国内在庫あり
1g	JPY 217000	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（20）

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製品安全説明書

現在のバッチを見る：純度： 99.90%

99.90

Clofarabine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

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
U373-MAGI	Function assay	50 nM	2 hrs	Potentiation of 5-Aza-C-induced antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as 5-Aza-C EC50 at 50 nM preincubated for 2 hrs followed by 5-Aza-C addition for 2 hrs and subsequent viral infection measu, EC50=30.4μM	27117260
U373-MAGI	Antiviral assay	50 nM	4 hrs	Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in viral infectivity at 50 nM incubated for 4 hrs prior to viral infection measured at 72 hrs post infection by flow cytometric analysis	27117260
U373-MAGI	Function assay	200 nM	6 hrs	Reduction in dGTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	200 nM	6 hrs	Reduction in dCTP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	200 nM	6 hrs	Reduction in dATP level in human U373-MAGI cells at 200 nM after 6 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	50 nM	2 hrs	Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	200 nM	2 hrs	Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-C	27117260
U373-MAGI	Function assay	50 nM	2 hrs	Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC	27117260
U373-MAGI	Function assay	200 nM	2 hrs	Increase in 5-aza-dCTP/dCTP ratio in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC	27117260
U373-MAGI	Function assay	200 nM	2 hrs	Reduction in dRGU-TP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	200 nM	2 hrs	Reduction in 5-aza-dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-C addition measured after 4 hrs by LC-MS/MS analysis	27117260
U373-MAGI	Function assay	200 nM	2 hrs	Reduction in dCTP level in human U373-MAGI cells at 200 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC	27117260
U373-MAGI	Function assay	50 nM	2 hrs	Reduction in dCTP level in human U373-MAGI cells at 50 nM preincubated for 2 hrs followed by 5-aza-dC addition measured after 4 hrs by LC-MS/MS analysis relative to 5-aza-dC	27117260
MT4	Cytostatic assay		5 days	Cytostatic activity against human MT4 cells after 5 days by SRB assay, GI50=0.051μM	21711054
NCI-H23	Cytostatic assay		5 days	Cytostatic activity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM	21711054
HCT15	Cytotoxicity assay		5 days	Cytotoxicity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM	19929004
BT549	Cytotoxicity assay		5 days	Cytotoxicity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM	19929004
PC3	Cytotoxicity assay		5 days	Cytotoxicity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM	19929004
NCI-H23	Cytotoxicity assay		5 days	Cytotoxicity against human NCI-H23 cells after 5 days by SRB assay, GI50=0.04μM	19929004
PC3	Cytostatic assay		5 days	Cytostatic activity against human PC3 cells after 5 days by SRB assay, GI50=0.063μM	21711054
BT549	Cytostatic assay		5 days	Cytostatic activity against human BT549 cells after 5 days by SRB assay, GI50=0.065μM	21711054
A549	Cytostatic assay		5 days	Cytostatic activity against human A549 cells after 5 days by SRB assay, GI50=0.086μM	21711054
HCT116	Cytostatic assay		5 days	Cytostatic activity against human HCT116 cells after 5 days by SRB assay, GI50=0.106μM	21711054
DU145	Cytostatic assay		5 days	Cytostatic activity against human DU145 cells after 5 days by SRB assay, GI50=0.125μM	21711054
HCT15	Cytostatic assay		5 days	Cytostatic activity against human HCT15 cells after 5 days by SRB assay, GI50=0.18μM	21711054
Hs578	Cytostatic assay		5 days	Cytostatic activity against human Hs578 cells after 5 days by SRB assay, GI50=1.241μM	21711054
HL60	Cytostatic assay		48 hrs	Cytostatic activity against human HL60 cells after 48 hrs by MTT assay, IC50=0.1μM	23820572
A549	Cytostatic assay		48 hrs	Cytostatic activity against human A549 cells after 48 hrs by MTT assay, IC50=8μM	23820572
Granta	Cytotoxicity assay		72 hrs	Cytotoxicity against human Granta cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.017μM	30176535
HL60	Cytotoxicity assay		72 hrs	Cytotoxicity against human HL60 cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.04μM	30176535
CCRF-CEM	Cytotoxicity assay		72 hrs	Cytotoxicity against human CCRF-CEM cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.044μM	30176535
RL	Cytotoxicity assay		72 hrs	Cytotoxicity against human RL cells assessed as decrease in cell viability after 72 hrs by MTT assay, IC50=0.38μM	30176535
L1210 cell	Cytotoxicity assay			Compound was tested for cytotoxicity against L1210 cell lines, IC50=2.3 μM	1732556
CCRF-CEM cell lines	Cytotoxicity assay			Compound was tested for cytotoxicity against CCRF-CEM cell lines, IC50=0.05 μM	1732556
HEp-2 cell	Cytotoxicity assay			Compound was tested for cytotoxicity against HEp-2 cell lines, IC50=0.012 μM	1732556
K562 cell	Cytotoxicity assay			Compound was tested for cytotoxicity against K562 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
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY 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
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 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
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 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
Rh30	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability screen for SJ-GBM2 cells	29435139
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Orthogonal 3D viability 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: Orthogonal 3D viability screen for MG 63 (6-TG R) cells	29435139
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生物活性

製品説明

Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis.

Targets

Ribonucleotide reductase ^[1]
(Cell-free assay)

65 nM

In Vitro
In vitro	Clofarabine is efficiently transported into cells via two facilitative or equilibrative nucleoside transporters, hENT1 and hENT2, and a concentrative nucleoside transporter, hCNT253. Clofarabine is phosphorylated in a stepwise manner by cytosolic kinases to the nucleotide analogues clofarabine 5′-mono-, di- and triphosphate following entry into cells, with Clofarabine triphosphate being the active form. Clofarabine 5′-mono-, di- and triphosphate are not substrates for nucleoside transporters and must be enzymatically converted by 5′-nucleotidase back to their dephosphorylated nucleoside form for transport out of the cell. Clofarabine triphosphate is a potent inhibitor of ribonucleotide reductase (IC50 = 65 nM), presumably by binding to the allosteric site on the regulatory subunit. Clofarabine has also been shown to act directly on mitochondria by altering the transmembrane potential with release of cytochrome c, apoptotic-inducing factor (AIF), apoptosis protease-activating factor 1 (APAF1) and caspase 9 into the cytosol. Clofarabine demonstrates strong in vitro growth inhibition and cytotoxic activity (IC50 values = 0.028–0.29 μM) in a wide variety of leukaemia and solid tumour cell lines. Clofarabine has been shown to increase the activity of dCK in HL60 cells, and increases the formation of the mono-, di-, and triphosphates of ara-C in K562 cells36. ^[1] Clofarabine (10 μM) inhibits the repair initiated by 4-hydroperoxycyclophosphamide (4-HC), with inhibition peaking at the intracellular concentrations of 5 μM in chronic lymphocytic leukemia (CLL) lymphocytes. Clofarabine (10 μM) combined with 4-hydroperoxycyclophosphamide (4-HC) produces more than additive apoptotic cell death than the sum of each alone. ^[2] Clofarabine (1 μM) combined with ara-C (10 μM) results in a biochemical modulation of ara-CTP and synergistic cell kill in K562 cells. ^[3]

In Vivo
In Vivo	Clofarabine administered intraperitoneally has significant activity against a wide variety of human tumour xenografts implanted subcutaneously in athymic nude or severe combined immune deficiency mice. ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05917405	Recruiting	Acute Myeloid Leukemia in Remission	Nantes University Hospital	September 14 2023	Phase 2
NCT03609814	Completed	Hematologic Malignancies\|Nonmalignant Diseases\|Immunodeficiencies\|Hemoglobinopathies\|Genetic Inborn Errors of Metabolism\|Fanconi''s Anemia\|Thalassemia\|Sickle Cell Disease	University of California San Francisco	January 26 2016	--

参考
[1] Bonate PL, et al. Nat Rev Drug Discov, 2006, 5(10), 855-863. [2] Yamauchi T, et al. Clin Cancer Res, 2001, 7(11), 3580-3589. [3] Cooper T, et al. Cancer Chemother Pharmacol, 2005, 55(4), 361-368.

参考

化学情報

分子量	303.68	化学式	C₁₀H₁₁ClFN₅O₃
CAS No.	123318-82-1	SDF	Download Clofarabine SDFをダウンロードする
Smiles	C1=NC2=C(N=C(N=C2N1C3C(C(C(O3)CO)O)F)Cl)N
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 : 60 mg/mL ( (197.57 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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