Lomustine - Moligand™, 10mM in DMSO , DNA inhibitor, CAS No.13010-47-4, DNA inhibitor

CAS: 13010-47-4 Cat. No.: L409232 Molecular Weight: 233.7 EC Number: 235-859-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

NSC79037, Gleostine, CeeNU, CCNU | N-​(2-​chloroethyl)​-​N'-​cyclohexyl-​N-​nitroso-urea

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging theDNAand stops cells from dividing.
In vitro

Lomustine inhibits the growth of ZR-75-1 and U373 with IC50 of 12 μM and 15 μM, respectively. Lomustine reduces the level of expression of the DNA repair protein O6-alkylguanine-DNA alkyltransferase. Lomustine (420 μM) triggers apoptosis through the mitochondrial pathway via decrease in the level of the anti-apoptosis proteins Bcl-2 and Bcl-xl, respectively, in both medulloblastoma and normal human epithelial and fibroblast cells. Lomustine induces cell cycle delay in G2/M phase in medulloblastoma cells and up-regulates p21 protein level in a p53-independent manner in HFSN1 cells.

In vivo

Lomustine can cause delayed, cumulative dose-related, chronic hepatotoxicity that is irreversible and can be fatal. Lomustine could result in infrequent severe hematological toxicity in cats with spontaneously arising tumors, and the incidence of either grade III or IV neutropenia and thrombocytopenia is 4.1% and 1.0%, respectively. Lomustine trends toward a greater likelihood for progressive neutropenia and statistically significant higher response rates in cats with spontaneously arising tumors.
Cell Data

cell lines：A375 cells

Concentrations：133 μM

Incubation Time：1 hour

Powder Purity:≥98%

Specifications

Synonyms

NSC79037, Gleostine, CeeNU, CCNU | N-​(2-​chloroethyl)​-​N'-​cyclohexyl-​N-​nitroso-urea

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Lomustine (NSC79037, Gleostine, CeeNU, CCNU) inhibits cancer cells by damaging the DNA and stops cells from dividing.

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: 2.8

Names and Identifiers

• Isomeric SMILES: C1CCC(CC1)NC(=O)N(CCCl)N=O
• WGK Germany: 3
• RTECS: YS4900000
• Molecular Weight: 233.7
• Reaxy-Rn: 2125058
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2125058&ln=

Chemical and Physical Properties

• Melt Point(°C): 89.0-93.0°C

References

1. Maryam H. Alaayedi, Nidhal K. Maraie.  (2023)  Lomustine’s nanoemulsion as nose-to-brain drug delivery system for CNS tumor treatment.  SAUDI PHARMACEUTICAL JOURNAL,      [PMID:37457367] [10.1016/j.jsps.2023.06.025]