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 Peso molecular: 303.68 Número EC: 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

Descripción general

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

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

INHIBITOR

Mecanismo de acción

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

Propiedades del producto

• ALogP: 0.9

Nombres e identificadores

• Isómeros SMILES: C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)F)Cl)N
• WGK Alemania: 2
• RTECS: UD7473000
• CAS alternativo: 123318-82-1
• Términos de entrada MeSH: 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
• Peso molecular: 303.68
• Reaxy-Rn: 24750214
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24750214&ln=

Objetivos asociados (humanos)

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)

Propiedades químicas y físicas

• Punto de fusión (°C): 227°C(lit.)