Clofarabine - Moligand™, 10mM in DMSO , Inhibitor of ribonucleotide reductase catalytic subunit M1;Inhibitor of ribonucleotide reductase regulatory subunit M2, CAS No.123318-82-1, Inhibitor of ribonucleotide reductase catalytic subunit M1;Inhibitor of ribonucleotide reductase regulatory subunit M2

CAS: 123318-82-1 Cat. No.: C408828 分子式: C₁₀H₁₁ClFN₅O₃ 分子量: 303.68 EC番号: 631-422-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Clolar | 2-​chloro-​9-​(2-​deoxy-​2-​fluoro-​β-​D-​arabinofuranosyl)​-9H-​purin-​6-​amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Clofarabine Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) ( IC50 = 65 nM) and DNA polymerase . Clofarabine induces autophagy and apoptosis .
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. 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. Clofarabine (1 μM) combined with ara-C (10 μM) results in a biochemical modulation of ara-CTP and synergistic cell kill in K562 cells.

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]
Cell Data

cell lines：A549 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

同義語

Clolar | 2-​chloro-​9-​(2-​deoxy-​2-​fluoro-​β-​D-​arabinofuranosyl)​-9H-​purin-​6-​amine

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

INHIBITOR

作用メカニズム

Inhibitor of ribonucleotide reductase catalytic subunit M1;Inhibitor of ribonucleotide reductase regulatory subunit M2

製品の性質

• ALogP: 0.9

名前と識別子

• 異性体SMILES: C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)F)Cl)N
• WGKドイツ: 2
• RTECS: UD7473000
• 代替CAS番号: 123318-82-1
• MeSH用語: 2 Chloro 2' arabino fluoro 2' deoxyadenosine;2 Chloro 2' fluoroarabino 2' deoxyadenosine;2-chloro-2'-arabino-fluoro-2'-deoxyadenosine;2-chloro-2'-fluoroarabino-2'-deoxyadenosine;2-chloro-9-(2-deoxy-2-fluoro-beta-D-arbinofuranosyl)adenine;2-chloro-9-(2-deo
• 分子量: 303.68
• Reaxy-Rn: 24750214
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24750214&ln=

関連ターゲット（人間）

RRM1 Tclin Ribonucleoside-diphosphate reductase large subunit (1 Activities)

Discover Target: RRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RRM2 Tclin Ribonucleoside-diphosphate reductase subunit M2 (1 Activities)

Discover Target: RRM2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 融点（°C）: 227°C(lit.)

よくある質問

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 123318-82-1, the molecular formula is C10H11ClFN5O3, and the molecular weight is 303.68 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.