Nelarabine - Moligand™, 10mM in DMSO , DNA inhibitor, CAS No.121032-29-9, DNA inhibitor

CAS: 121032-29-9 Cat. No.: N409145 Formula: C₁₁H₁₅N₅O₅ Molecular Weight: 297.27 EC Number: 642-916-9

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

506U78 | 9-​β-​D-​arabinofuranosyl-​6-​methoxy-9H-​purin-​2-​amine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Nelarabine Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
In vitro

The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively. Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity.

In vivo

The Nelarabine plasma AUC is 2.82 mM minutes and the ara-G plasma AUC is 20 mM minutes. The terminal half-life of Nelarabine in plasma is 25 min, clearance is 42 mL/minutes/kg, and central volume of distribution is 1.1 L/kg. The terminal half-life of ara-G in plasma is 182 minutes and the central volume of distribution is 1.4 L/kg. In CSF the terminal half-life of Nelarabine is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for Nelarabine and 23 % for ara-G. Nelarabine and ara-G do not accumulate with daily infusions because of their relatively short half-lives.
Cell Data

cell lines：

Concentrations：0.125 μg/mL - 8 μg/mL

Incubation Time：96 hours

Powder Purity:≥99%

Specifications

Synonyms

506U78 | 9-​β-​D-​arabinofuranosyl-​6-​methoxy-9H-​purin-​2-​amine

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

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.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

DNA inhibitor

Product Properties

• alogp: -0.7

Names and Identifiers

• Isomeric SMILES: COC1=NC(=NC2=C1N=CN2[C@H]3[C@H]([C@@H]([C@H](O3)CO)O)O)N
• Molecular Weight: 297.27
• Reaxy-Rn: 841479
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=841479&ln=

References

1. Kangkang Wang, Yuli Kou, Meng Wang, Xin Ma, Jide Wang.  (2020)  Determination of Nitrofuran Metabolites in Fish by Ultraperformance Liquid Chromatography-Photodiode Array Detection with Thermostatic Ultrasound-Assisted Derivatization.  ACS Omega,      [PMID:32775890] [10.1021/acsomega.0c02068]