Fludarabine Phosphate - 10mM in DMSO , Ribonucleoside-diphosphate reductase RR1 inhibitor, CAS No.75607-67-9, Ribonucleoside-diphosphate reductase RR1 inhibitor

CAS: 75607-67-9 Cat. No.: F408811 Molecular Weight: 365.21 EC Number: 616-242-0

GRADE & PURITY 10mM in DMSO

Synonyms

F-ara-A (NSC 312887) Phosphate | 2-​fluoro-​9-​(5-​O-​phosphono-​β-​D-​arabinofuranosyl)​-9H-​purin-​6-​amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Fludarabine Phosphate Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
In vitro

Fludarabine Phosphate is converted to F-ara-ATP in cells and then incorporated into DNA in a self-limiting manner. Fludarabine Phosphate competes with dATP for incorporation into the A site of the extending DNA strand, which results in termination of DNA strand elongation. Human DNA polymerase α incorporates more Fludarabine Phosphate into DNA than polymerase δ. Fludarabine Phosphate completively inhibits DNA polymerase α and DNA polymerase δ with K_i of 1.1 μM and 1.3 μM, respectively. DNA polymerase δ is also able to excise the incorporated Fludarabine Phosphate from DNA in vitro.

In vivo

Fludarabine Phosphate is toxic for tumor-free mice. The maximum tolerated dose (LD10) Fludarabine Phosphate administered as a single dose is 234 mg/kg. The 50% lethal dose is 375 mg/kg. Fludarabine Phosphate administered as a single dose induces fewer number of cells surviving therapy in mice bearing P388 leukemia, accompanied by greater percentage of increase in life span (110%) and increased median survival time.
Cell Data

cell lines：

Concentrations：30 μM

Incubation Time：5 hours

Powder Purity:≥99%

Specifications

Synonyms

F-ara-A (NSC 312887) Phosphate | 2-​fluoro-​9-​(5-​O-​phosphono-​β-​D-​arabinofuranosyl)​-9H-​purin-​6-​amine

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Fludarabine Phosphate (F-ara-A, NSC 312887) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Mechanism of action

Ribonucleoside-diphosphate reductase RR1 inhibitor

Product Properties

• ALogP: -3.1

Names and Identifiers

• Isomeric SMILES: C1=NC2=C(N=C(N=C2N1[C@H]3[C@H]([C@@H]([C@H](O3)COP(=O)(O)O)O)O)F)N
• WGK Germany: 3
• RTECS: UO7440900
• Molecular Weight: 365.21
• Reaxy-Rn: 24865932
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24865932&ln=

Associated Targets(Human)

CA5A Tclin Carbonic anhydrase 5A, mitochondrial (1 Activities)

Discover Target: CA5A

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

Chemical and Physical Properties

• Specific Rotation[α]: 12° (C=0.5,H2O)
• Melt Point(°C): 203°C(dec.)(lit.)