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Lomustine

Catalog No. T1601   CAS 13010-47-4
Synonyms: CCNU, NSC 79037

Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.

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Lomustine Chemical Structure
Lomustine, CAS 13010-47-4
Pack Size Availability Price/USD Quantity
100 mg In stock $ 50.00
200 mg In stock $ 85.00
1 mL * 10 mM (in DMSO) In stock $ 50.00
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Purity: 99.86%
Purity: 98.36%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Lomustine (NSC-79037) is an alkylating agent of value against both hematologic malignancies and solid tumors.
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. [1] 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. [2]
In vivo Lomustine can cause delayed, cumulative dose-related, chronic hepatotoxicity that is irreversible and can be fatal. [4] 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. [5]
Cell Research Cell lines are routinely grown as monolayers in DMEM supplemented with 10% foetal calf serum, 25 mm HEPES, glutamine and penicillin/streptomycin. Cytotoxicity studies are carried out in HEPES-free medium in a 5% CO2 atmosphere. 750-1000 cells/well are plated in 96 well plates and after overnight incubation are treated for 2 hours with or without 33 μM BG. Temozolomide or CCNU is then added for 1 hour in the same medium, the final DMSO concentration not exceeding 1%. The cells are grown for a further 7 days in fresh medium and assayed for protein content by the NCI sulphorhodamine assay; growth studies show that cells are in log phase growth during the assay period. For the repeat temozolomide dosing schedule cells are given consecutive 24 hours treatments, with fresh medium each day. Assays are carried out at least in duplicate.(Only for Reference)
Synonyms CCNU, NSC 79037
Molecular Weight 233.7
Formula C9H16ClN3O2
CAS No. 13010-47-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 42 mg/mL(179.7 mM)

TargetMolReferences and Literature

1. Baer JC, et al. Br J Cancer, 1993, 67(6), 1299-12302. 2. Shinwari Z, et al. J Neurooncol, 2008, 87(2), 123-132. 3. Rassnick KM, et al. J Vet Intern Med, 1999, 13(6), 601-605. 4. Kristal O, et al. J Vet Intern Med, 2004, 18(1), 75-80. 5. Fan TM, et al. J Am Anim Hosp Assoc, 2002, 38(4), 357-363. 6. Wang P, et al. Oncometabolite D-2-Hydroxyglutarate Inhibits ALKBH DNA Repair Enzymes and Sensitizes IDH Mutant Cells to Alkylating Agents. Cell Rep. 2015 Dec 22;13(11):2353-2361. 7. Harvey KA, et al. Enhanced anticancer properties of lomustine in conjunction with docosahexaenoic acid in glioblastoma cell lines. J Neurosurg. 2015 Mar;122(3):547-56. 8. Yagiz K, et al. Toca 511 plus 5-fluorocytosine in combination with lomustine shows chemotoxic and immunotherapeutic activity with no additive toxicity in rodent glioblastoma models. Neuro Oncol. 2016 Oct;18(10):1390-401.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Tyrosine Kinase Inhibitor Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Anti-Aging Compound Library Hematopoietic Toxicity Compound Library Pediatric Drug Library NO PAINS Compound Library Orally Active Compound Library

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Keywords

Lomustine 13010-47-4 Apoptosis Autophagy DNA Damage/DNA Repair Others DNA Alkylation DNA Alkylator/Crosslinker inhibit NSC79037 NSC-79037 Inhibitor CCNU NSC 79037 inhibitor

 

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